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阻害剤

天然化合物

カタログ番号	製品名	別名	ターゲット
T64414	PRI-724	C-82 prodrug,Foscenvivint	Wnt/beta-catenin
	PRI-724 (C-82 prodrug) is a selective small-molecule inhibitor of β-catenin/CBP interaction.		Wnt/beta-catenin
T72406	Tofacitinib Prodrug-1
	Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low ...
T64076	Spermine Prodrug-1
	Spermine Prodrug-1 is a redox-sensitive spermine prodrug. Spermine Prodrug-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblasts with IC50 values of 326.7. 198.5, ...
T3934	Isavuconazonium sulfate		Antifungal
	Isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), wh...		Antifungal
T33281	Melflufen	Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1
	Melphalen fluoroaniline, also known as melphalen, J-1, or prodrug J-1, is a prodrug of melphalen, in which the alkylating agent melphalen is combined with fluoroaniline and has potential antitumor and antiangiogenic acti...
T0103	Dipivefrin hydrochloride	Dipivefrin HCL	Adrenergic Receptor , AChR
	Dipivefrin hydrochloride (Dipivefrin HCl) that is available as an ophthalmic solution is a prodrug of adrenaline, which is used to treat glaucoma.		Adrenergic Receptor , AChR
T15102	Dexamethasone palmitate	DXP	Glucocorticoid Receptor
	Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone, shows a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Dexamethasone palmitate is a glucocorticoid receptor agonist and an...		Glucocorticoid Receptor
T19438	Myristyl nicotinate	Tetradecyl nicotinate	GPR
	Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivery of nicotinic acid (NIC) into the skin for prevention of actinic keratosis and its progression to skin cancer.		GPR
T0389	Dabigatran etexilate	BIBR 1048	Thrombin
	Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor, which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation.		Thrombin
T7840	2',3',5'-triacetyl-5-Azacytidine	Nsc291930	DNA Methyltransferase , Others
	2',3',5'-triacetyl-5-Azacytidine (Nsc291930) is a prodrug form of 5-azacytidine that may be rapidly absorbed orally.		DNA Methyltransferase , Others
T1579	Mestranol	Devocin,Norquen,Menophase	Estrogen Receptor/ERR , Estrogen/progestogen Receptor
	Mestranol (Devocin), a semisynthetic estrogen, is used as an estrogen receptor agonist and must be demethylated to be biologically active.		Estrogen Receptor/ERR , Estrogen/progestogen Receptor
T13278	Valecobulin hydrochloride	CKD-516 hydrochloride	Microtubule Associated
			Microtubule Associated
T40475	Ceftobiprole medocaril	BAL5788	Antibacterial
	Ceftobiprole medocaril (BAL5788) is the parenteral prodrug of Ceftobiprole. Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA).		Antibacterial
TQ0095	Brincidofovir	CMX001,HDP-CDV	Others , Antiviral , HSV
	Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir. It has enhanced activity compared to CDV against certain adenoviruses, herpesviruses, and orthopoxviruses.		Others , Antiviral , HSV
T1675	Adefovir dipivoxil	Hepsera,GS 0840,Preveon	Others , HBV , Reverse Transcriptase
	Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficienc...		Others , HBV , Reverse Transcriptase
T4190	Ticlopidine	PCR 5332,Ticlid	ATPase , Adiponectin receptor
	Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.		ATPase , Adiponectin receptor
T5133	Dabigatran Etexilate Mesylate	BIBR 1048MS,Dabigatran etexilate methanesulfonate	Thrombin
	Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).		Thrombin
T7387	Ceftaroline fosamil	TAK-599,PPI0903	Antibacterial , Antibiotic
	Ceftaroline fosamil (TAK-599) is a cephalosporin, with activity against Gram-positive pathogens.		Antibacterial , Antibiotic
T2305	Isavuconazole	BAL-4815,RO-0094815	P450 , Antibiotic , Antifungal
	Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabr...		P450 , Antibiotic , Antifungal
T24047	Etilevodopa hydrochloride	Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester	Others , Dopamine Receptor , Drug Metabolite
	Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.		Others , Dopamine Receptor , Drug Metabolite
T1142	Clindamycin phosphate	Clindamycin 2-phosphate,Clindamycin 2-dihydrogen phosphate,NSC 618653,U-28508	ribosome , Antibacterial , Antibiotic , Parasite
	Clindamycin Phosphate is the phosphate salt form of clindamycin, a semi-synthetic, chlorinated broad-spectrum antibiotic produced by chemical modification of lincomycin. Clindamycin phosphate (Clindamycin 2-dihydrogen ph...		ribosome , Antibacterial , Antibiotic , Parasite
T5954	Methyldopa hydrate	Alpha-Methyldopa Sesquihydrate,L-(-)-α-Methyldopa hydrate,MK-351 hydrate,Methyldopa Sesquihydrate	Dopamine Receptor , Adrenergic Receptor
	Methyldopa hydrate (MK-351 hydrate) is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension. It inhibits the sympathetic nervous system, decreases production of dopamine, ...		Dopamine Receptor , Adrenergic Receptor
T3085	Piperacetazine	Psymod,Piperacetazinum,Quide	Dopamine Receptor , 5-HT Receptor
	Piperacetazine (Piperacetazinum), an antipsychotic prodrug, is used forschizophrenia.		Dopamine Receptor , 5-HT Receptor
T17218	Varespladib methyl	A-002,LY333013	Others , Phospholipase
	Varespladib methyl (LY333013), a bioavailable prodrug of Varespladib, is a selective group II secretory phospholipase A2 inhibitor.		Others , Phospholipase
T24540	NO-711ME	NO711ME,NO711 Methyl ester,N-O711 Methyl ester,N O711 Methyl ester	GABA Receptor
	NO-711ME (N-O711 Methyl ester) is a prodrug of NO-711. It also is a potent and selective GABA uptake inhibitor.		GABA Receptor
T5328	Fosfluconazole		Antifungal
	Fosfluconazole is water-soluble phosphate prodrug of fluconazole. Fluconazole is an antifungal drug.		Antifungal
T16716	Rabacfosadine	VDC-1101,GS-9219	Others
	Rabacfosadine (GS-9219) is a novel prodrug of PMEG, an acyclic nucleotide phosphonate, with antitumor activity for the study of lymphoma.		Others
T9472	Rebamipide mofetil		COX
	Rebamipide mofetil is an orally active prodrug of Rebamipide which is a mucoprotective agent.		COX
T7854	Bortezomib-pinanediol		Proteasome
	Bortezomib-pinanediol is a proteasome inhibitor. is a prodrug of Bortezomib.		Proteasome
T23667	AGN-201904	AGN201904,AGN 201904	ATPase
	AGN-201904 is a proton pump inhibitor, an omeprazole prodrug, which delays aging and may be used for the prevention and treatment of peptic ulcers.		ATPase
T39476	NLG802		Indoleamine 2,3-Dioxygenase (IDO)
	NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.		Indoleamine 2,3-Dioxygenase (IDO)
T8238	Fosamprenavir Calcium Salt	Diallyl Trisulfide,GW433908G	HIV Protease
	Fosamprenavir Calcium Salt (GW433908G) (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Fosamprenavir Calcium Salt has Anti-HIV infection.		HIV Protease
T2419	BMS-794833		VEGFR , c-Met/HGFR
	BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2; a prodrug of BMS-817378.		VEGFR , c-Met/HGFR
T40276	GS-621763		SARS-CoV
	GS-621763, a prodrug of GS-441524, exhibits antiviral activity against SARS-CoV-2 pathogenesis.		SARS-CoV
T5186	Oseltamivir acid	GS 4071,oseltamivir carboxylate,Ro 64-0802	Influenza Virus , Drug Metabolite
	Oseltamivir acid (GS4071) is a potent influenza virus neuraminidase inhibitor and the prodrug of GS4071.		Influenza Virus , Drug Metabolite
T36526	IL-17 modulator 4		Interleukin
	IL-17 modulator 4 is a prodrug of IL-17 modulator 1 which is an efficacious modulator of IL-17.		Interleukin
T13365	YHO-13351 free base		BCRP
	YHO-13351 free base is the water-soluble prodrug of YHO-13177 which is an inhibitor of BCRP .		BCRP
T68120L	Ot-730 HCl	Ot-730 HCl(870809-51-1 Free base)	Others
	ot-730 HCl is a novel selective beta blocker prodrug for the study of ocular diseases.		Others
T4061	LY2334737		Nucleoside Antimetabolite/Analog , Others , Virus Protease
	LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.		Nucleoside Antimetabolite/Analog , Others , Virus Protease
T26686	AV-101	L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine	NMDAR
	AV-101 (4-Cl-KYN) , a prodrug antagonist at the glycine site of the NMDA receptor, has antidepressant activity and reduces levodopa-induced dyskinesia in MPTP monkeys.		NMDAR
T1645	Ramipril	HOE-498,Tritace,Altace,Carasel	Apoptosis , RAAS
	Ramipril (Altace) is a long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.		Apoptosis , RAAS
T6998	Tedizolid Phosphate	TR-701FA,Torezolid phosphate	Antibacterial , Antibiotic
	Tedizolid Phosphate (TR-701FA) is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid.		Antibacterial , Antibiotic
T68120	Ot-730	QLT 091568	Others
	ot-730（QLT 091568） is a new selective beta blocker prodrug that can be used to study eye diseases.		Others
T16018	MB-07811	VK-2809	Thyroid hormone receptor(THR)
	MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344 with cholesterol and triglycerides lowering activity. MB-07811 is an agonist of liver-targeted THR-β.		Thyroid hormone receptor(THR)
T13038	Sultamicillin		Antibacterial , Antibiotic
	Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic β-Lactamase inhibitor.		Antibacterial , Antibiotic
T1087	Valacyclovir hydrochloride	Valaciclovir hydrochloride,Valaciclovir HCl	DNA/RNA Synthesis , Antibiotic , HSV
	Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an acyclovir prodrug that inhibits viral DNA replication after metabolization.		DNA/RNA Synthesis , Antibiotic , HSV
T7282	Tenofovir alafenamide hemifumarate	GS-7340 (hemifumarate),Tenofovir alafenamide fumarate	HIV Protease , Reverse Transcriptase
	Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV)		HIV Protease , Reverse Transcriptase
T2409	Tenofovir alafenamide	GS-7340	HIV Protease , Reverse Transcriptase
	Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.		HIV Protease , Reverse Transcriptase
T7066	Fosphenytoin disodium	Fosphenytoin sodium,ACC-9653	Sodium Channel
	Fosphenytoin disodium (ACC-9653) is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker		Sodium Channel
T22304	Desciclovir	BW A515U,6-Deoxyacyclovir,DCV	Antifection
	Desciclovir (DCV), a prodrug of the antiherpetic agent acyclovir (ACV), is converted in humans to ACV, presumably by xanthine oxidase.		Antifection

Compounds

PRI-724

T64414

Synonym: C-82 prodrug,Foscenvivint

Target: Wnt/beta-catenin

Tofacitinib Prodrug-1

Isavuconazonium sulfate

Synonym: Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1

Target:

Dipivefrin hydrochloride

T0103

Synonym: Dipivefrin HCL

Target: Adrenergic Receptor, AChR

Dexamethasone palmitate

T15102

Synonym: DXP

Target: Glucocorticoid Receptor

Myristyl nicotinate

T19438

Synonym: Tetradecyl nicotinate

2',3',5'-triacetyl-5-Azacytidine

T7840

Synonym: Nsc291930

Target: DNA Methyltransferase, Others

Mestranol

T1579

Synonym: Devocin,Norquen,Menophase

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Valecobulin hydrochloride

T13278

Synonym: CKD-516 hydrochloride

Target: Microtubule Associated

Ceftobiprole medocaril

T40475

Synonym: BAL5788

Target: Antibacterial

Brincidofovir

TQ0095

Synonym: CMX001,HDP-CDV

Target: Others, Antiviral, HSV

Adefovir dipivoxil

T1675

Synonym: Hepsera,GS 0840,Preveon

Target: Others, HBV, Reverse Transcriptase

Ticlopidine

T4190

Synonym: PCR 5332,Ticlid

Target: ATPase, Adiponectin receptor

Dabigatran Etexilate Mesylate

T5133

Synonym: BIBR 1048MS,Dabigatran etexilate methanesulfonate

Target: Thrombin

Ceftaroline fosamil

T7387

Synonym: TAK-599,PPI0903

Target: Antibacterial, Antibiotic

Isavuconazole

T2305

Synonym: BAL-4815,RO-0094815

Target: P450, Antibiotic, Antifungal

Etilevodopa hydrochloride

T24047

Synonym: Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester

Target: Others, Dopamine Receptor, Drug Metabolite

Clindamycin phosphate

T1142

Synonym: Clindamycin 2-phosphate,Clindamycin 2-dihydrogen phosphate,NSC 618653,U-28508

Target: ribosome, Antibacterial, Antibiotic, Parasite

Methyldopa hydrate

T5954

Synonym: Alpha-Methyldopa Sesquihydrate,L-(-)-α-Methyldopa hydrate,MK-351 hydrate,Methyldopa Sesquihydrate

Target: Dopamine Receptor, Adrenergic Receptor

Piperacetazine

T3085

Synonym: Psymod,Piperacetazinum,Quide

Target: Dopamine Receptor, 5-HT Receptor

Varespladib methyl

T17218

Synonym: A-002,LY333013

Target: Others, Phospholipase

NO-711ME

T24540

Synonym: NO711ME,NO711 Methyl ester,N-O711 Methyl ester,N O711 Methyl ester

Target: GABA Receptor

Synonym: VDC-1101,GS-9219

Bortezomib-pinanediol

Synonym: AGN201904,AGN 201904

Target: Indoleamine 2,3-Dioxygenase (IDO)

Fosamprenavir Calcium Salt

T8238

Synonym: Diallyl Trisulfide,GW433908G

Target: VEGFR, c-Met/HGFR

Synonym: GS 4071,oseltamivir carboxylate,Ro 64-0802

Target: Influenza Virus, Drug Metabolite

Synonym: Ot-730 HCl(870809-51-1 Free base)

Target: Nucleoside Antimetabolite/Analog, Others, Virus Protease

AV-101

T26686

Synonym: L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine

Target: NMDAR

Ramipril

T1645

Synonym: HOE-498,Tritace,Altace,Carasel

Target: Apoptosis, RAAS

Tedizolid Phosphate

T6998

Synonym: TR-701FA,Torezolid phosphate

Target: Antibacterial, Antibiotic

Target: Thyroid hormone receptor(THR)

Sultamicillin

T13038

Synonym:

Target: Antibacterial, Antibiotic

Valacyclovir hydrochloride

T1087

Synonym: Valaciclovir hydrochloride,Valaciclovir HCl

Target: DNA/RNA Synthesis, Antibiotic, HSV

Tenofovir alafenamide hemifumarate

T7282

Synonym: GS-7340 (hemifumarate),Tenofovir alafenamide fumarate

Target: HIV Protease, Reverse Transcriptase

Tenofovir alafenamide

T2409

Synonym: GS-7340

Target: HIV Protease, Reverse Transcriptase

Fosphenytoin disodium

T7066

Synonym: Fosphenytoin sodium,ACC-9653

Target: Sodium Channel

Desciclovir

T22304

Synonym: BW A515U,6-Deoxyacyclovir,DCV

Target: Antifection

カタログ番号	製品名	別名	ターゲット
TC0025	Testosterone acetate	NSC523836,NSC-523836,NSC 523836	Others
	Testosterone acetate (NSC-523836) is a hormone with in vitro antitumor activity.		Others
T8160	EGCG Octaacetate		Others , Antibacterial
	EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.		Others , Antibacterial
T19676	Tributyrin	NSC661583,NSC 661583,NSC-661583	Apoptosis
	Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracell...		Apoptosis
T0505	Methyldopa	L-(-)-α-Methyldopa,MK-351	Dopamine Receptor , Adrenergic Receptor
	Methyldopa (MK-351), an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive medicine, is served as an antihypertensive or sympatholytic.		Dopamine Receptor , Adrenergic Receptor
T0132	Etoposide	VP-16,VP-16-213	Apoptosis , Mitophagy , Topoisomerase , Antibacterial , Antibiotic , Autophagy
	Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.
TN7246	3-Sulfopropanoic acid	3-SPA	Drug Metabolite
	3-Sulfopropanoic acid, a major metabolite of treprostinil and its prodrug ALZ-801, is an endogenous molecule present in the cerebrospinal fluid (CSF) of AD patients that inhibits the formation of Aβ42 oligomers.		Drug Metabolite
T3S2007	MRE-269	MRE 269,ACT-333679,MRE269	Prostaglandin Receptor
	MRE-269 (ACT-333679) is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269(ACT-333679) is used for the treatment of pulmonary arterial hypertension. MRE-269(ACT-333679) is an active metabo...		Prostaglandin Receptor
T6272	Fosbretabulin Disodium	Combretastatin A4 Phosphate,CA 4DP,CA 4P,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium	Apoptosis , Microtubule Associated
	Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibit...		Apoptosis , Microtubule Associated
T1273	Diacerein	Diacerhein,Fisiodar,Diacetylrhein	IL Receptor , Interleukin
	Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre ...		IL Receptor , Interleukin
T1591	Ancitabine hydrochloride	NSC 145668 HCl,Cyclocytidine hydrochloride,Cyclo-CMP hydrochloride,Cyclocytidine HCl,Cyclo-C	Others , DNA/RNA Synthesis , Autophagy
	Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytar...		Others , DNA/RNA Synthesis , Autophagy
T0486L	Irinotecan Hydrochloride	Camptothecin 11 hydrochloride,CPT-11 hydrochloride	Topoisomerase , Autophagy
	Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptoth...		Topoisomerase , Autophagy
T0848	L-DOPA	Levodopa,3,4-Dihydroxyphenylalanine	Dopamine Receptor , Endogenous Metabolite
	L-DOPA (Levodopa) is an amino acid precursor of dopamine with antiparkinsonian properties. Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. When in the brai...		Dopamine Receptor , Endogenous Metabolite
T20976	Clostebol acetate	Clostebolacetate,Clostene,Alfa-Trofodermin,4-CLTA
	Clostebol acetate is a synthetic anabolic-androgenic steroid (AAS) and a derivative of testosterone. It acts as a prodrug of clostebol in the body.
T15255	Etilevodopa	Levodopa ethyl ester,L-DOPA ethyl ester	Others
	Etilevodopa is an ethyl-ester prodrug of Levodopa which is used for the treatment of Parkinson's disease (PD). It is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Levo...		Others