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天然化合物

カタログ番号	製品名	別名	ターゲット
T16369	O-Desmethyl gefitinib		EGFR
	O-Desmethyl gefitinib inhibits EGFR (IC50: 36 nM in subcellular assays). In human plasma, O-Desmethyl gefitinib is an active metabolite of Gefitinib. The formation of O-desmethyl gefitinib is dependent on the CYP2D6 acti...		EGFR
T28827	Sofpironium bromide	BBI4000,BBI 4000,BBI-4000	Others , AChR
	Sofpironium bromide (BBI4000) belongs to a class of drugs called anticholinergics, which exert their effect by blocking the action of acetylcholine.		Others , AChR
T10989	Dehydroaripiprazole	OPC-14857,DM-14857	5-HT Receptor
	Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has anti...		5-HT Receptor
T10335	Antihistamine-1		P450
	Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).		P450
T34795	Tedatioxetine	Lu AA 24530,Lu AA-24530,Lu AA24530	Dopamine Receptor , Serotonin Transporter
	Tedatioxetine (Lu AA24530) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) with antidepressant properties.Tedatioxetine acts as a CYP2D6 substrate.		Dopamine Receptor , Serotonin Transporter
T4281	Endoxifen	(E/Z)-N-desmethyl-4-hydroxy Tamoxifen,(E/Z)-Endoxifen	Estrogen Receptor/ERR , Aromatase , Estrogen/progestogen Receptor , Parasite , Drug Metabolite
	(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-f...
T8182L	Guan-fu base A hydrochloride(1394-48-5 free base)		P450
	Guan-fu base A hydrochloride is an antiarrhythmic alkaloid was isolated from Aconitum coreanum. Guanfu base A is hydrochloride a CYP2D6 inhibitor of human, monkey, and dog isoforms.		P450
T1443	Memantine hydrochloride	Namenda,Memantine HCl,D-145 (hydrochloride)	P450 , GluR , NMDAR , Autophagy , iGluR
	Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.		P450 , GluR , NMDAR , Autophagy , iGluR
T7788	2-Phenyl-2-(1-piperidinyl)propane		Others
	2-Phenyl-2-(1-piperidinyl)propane (PPP), an analog of phencyclidine		Others
T4488	GSK-25	GSK25	ROCK , S6 Kinase , mTOR
	GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).		ROCK , S6 Kinase , mTOR
T50001	Tinoridine	ethyl 2-amino-6-benzyl-4H,5H,6H,7H-thieno[2,3-c]pyridine-3-carboxylate	P450
	Tinoridine is a quinoline derivative analog that acts by inhibiting the production of cyclooxygenase-2 (COX-2). It has anti-inflammatory, anti-allergic and anticoagulant activities.		P450
T68531	MCV-4527 hydrochloride
	MCV-4527 hydrochloride is a new designer drug used as a potent inhibitor of CYP2D6.
T71926	Melperone hydrochloride
	Melperone hydrochloride is a butyrophenone neuroleptic and an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine.
T69094	α-hydroxy Metoprolol
	α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol. It is formed via metabolism of metoprolol by the cytochrome P450 (CYP) isoform CYP2D6.
T83896	Promethazine Sulfoxide
	Promethazine sulfoxide, a metabolite of the histamine H1 receptor antagonist promethazine, is produced via the action of the cytochrome P450 (CYP) isoform CYP2D6, converting promethazine into this compound.
T82194	HIV-IN-9
	HIV-IN-9 (Compound 2b) is an HIV inhibitor with an IC50 value of 6.65 μg/mL, demonstrating high binding affinity for HIV-RT. Additionally, it inhibits the cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C1, and CYP2D6 [1]...
T10144	4-Hydroxyatomoxetine D3		Others
	4-Hydroxyatomoxetine D3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inh...		Others
T12806	(S)-Mirtazapine D3	(S)-Org3770 D3,(S)-6-Azamianserin D3	5-HT Receptor
	(S)-Mirtazapine D3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a stereoselective antagonist of 5-HT2 receptor. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.		5-HT Receptor
T10145	4-Hydroxyatomoxetine		Others
	4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.		Others
T21684	Bufuralol (hydrochloride)
	Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity, which is also a CYP2D6 probe substrate [1] [2].
T37360	6-O-desmethyl Donepezil
	6-O-desmethyl Donepezil is an active metabolite of the acetylcholinesterase inhibitor donepezil . It is formed through dealkylation by the cytochrome P450 (CYP) isoform CYP2D6. It inhibits human ether a go-go (hERG) chan...
T36664	Dehydro Aripiprazole (hydrochloride)
	Dehydro aripiprazole is the primary, active metabolite of aripiprazole, an atypical antipsychotic. The metabolite is produced from the parent compound by the actions of cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6. D...
T61515	5-HT7 receptor ligand 1
	5-HT7 receptor ligand 1 (Compound 5c) is a potent ligand for the 5-HT7 receptor, with a K i value of 8 nM. The compound demonstrates non-hepatotoxic properties and displays moderate potential for drug-drug interactions w...
T70786	ML252
	ML252 is a selective potassium channel inhibitor, specifically targeting the KCNQ2 channel (Kv7.2) with an IC50 value of 69 nM. Additionally, ML252 demonstrates inhibitory activity against Cytochrome P450 isoforms, inclu...
TMIH-0402	O-Desmethyl Gefitinib-d8
	O-Desmethyl Gefitinib-d8 is a deuterated compound of O-Desmethyl Gefitinib. O-Desmethyl Gefitinib has a CAS number of 847949-49-9. O-Desmethyl gefitinib inhibits EGFR (IC50: 36 nM in subcellular assays). In human plasma,...
T37211	5-hydroxy-6-methoxy (S)-Duloxetine
	5-hydroxy-6-methoxy (S)-Duloxetine is a metabolite of (S)-duloxetine . It is formed from (S)-duloxetine via a 5- or 6-hydroxy duloxetine intermediate, which is formed by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2...
T38131	(E)-10-Hydroxynortriptyline
	(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline . Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1...
T71578	Endoxifen mesylate
	Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and ot...
T83888	(S)-5-hydroxy-6-methoxy Duloxetine maleate
	(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A...
T79754	JNK-IN-14		JNK
	JNK-IN-14 is a potent inhibitor of JNK with IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3. It induces early-stage apoptosis, arrests cell population at the G2/M phase, and moderately inhibits be...		JNK
T15048	Dagrocorat	PF-00251802	Others
	Dagrocorat is a novel and dissociated agonist of glucocorticoid receptor.		Others
T10535	BI 653048		P450
	BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.		P450
T10535L	BI 653048 phosphate		P450
	BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).		P450
T16097	MK-8318		Others
	MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).		Others

Compounds

O-Desmethyl gefitinib

Synonym: BBI4000,BBI 4000,BBI-4000

Target: Others, AChR

Dehydroaripiprazole

T10989

Synonym: OPC-14857,DM-14857

Target: 5-HT Receptor

Synonym: Lu AA 24530,Lu AA-24530,Lu AA24530

Target: Dopamine Receptor, Serotonin Transporter

Endoxifen

T4281

Synonym: (E/Z)-N-desmethyl-4-hydroxy Tamoxifen,(E/Z)-Endoxifen

Target: Estrogen Receptor/ERR, Aromatase, Estrogen/progestogen Receptor, Parasite, Drug Metabolite

Guan-fu base A hydrochloride(1394-48-5 free base)

T8182L

Synonym:

Target: P450

Memantine hydrochloride

T1443

Synonym: Namenda,Memantine HCl,D-145 (hydrochloride)

Target: P450, GluR, NMDAR, Autophagy, iGluR

2-Phenyl-2-(1-piperidinyl)propane

Target: ROCK, S6 Kinase, mTOR

Tinoridine

T50001

Synonym: ethyl 2-amino-6-benzyl-4H,5H,6H,7H-thieno[2,3-c]pyridine-3-carboxylate

Target: P450

MCV-4527 hydrochloride

T68531

Synonym:

Target:

Melperone hydrochloride

Promethazine Sulfoxide

4-Hydroxyatomoxetine D3

Synonym: (S)-Org3770 D3,(S)-6-Azamianserin D3

Target: 5-HT Receptor

Bufuralol (hydrochloride)

T21684

Synonym:

Target:

6-O-desmethyl Donepezil

T37360

Synonym:

Target:

Dehydro Aripiprazole (hydrochloride)

T36664

Synonym:

Target:

5-HT7 receptor ligand 1

O-Desmethyl Gefitinib-d8

TMIH-0402

Synonym:

Target:

5-hydroxy-6-methoxy (S)-Duloxetine

T37211

Synonym:

Target:

(E)-10-Hydroxynortriptyline

(S)-5-hydroxy-6-methoxy Duloxetine maleate

カタログ番号	製品名	別名	ターゲット
T10835	Cletoquine	Desethylhydroxychloroquine	Parasite , Antifection
	Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatme...		Parasite , Antifection
T8182	Guanfu base A	Guan-fu base A	P450 , Potassium Channel , HER
	Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.		P450 , Potassium Channel , HER
TQ0296L	N-Nornuciferine hydrochloride(4846-19-9 free base)	N-Nornuciferine hydrochloride	P450
	N-Nornuciferine hydrochloride(4846-19-9 free base) (N-Nornuciferine hydrochloride) is an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).		P450
T3401	Ginsenoside F1	20(S)-Ginsenoside F1	P450 , Endogenous Metabolite
	Ginsenoside F1 (20(S)-Ginsenoside F1) is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of the activity of CYP2D6.		P450 , Endogenous Metabolite
T2878	Ginsenoside Rd	Panaxoside Rd,Sanchinoside Rd,Gypenoside VIII	P450 , Calcium Channel , NF-κB , COX , Endogenous Metabolite
	Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors.
T5S2361	Epiberberine		ERK , Beta-Secretase , MEK , BACE , AMPK , AChR , AChE
	1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte diffe...		ERK , Beta-Secretase , MEK , BACE , AMPK , AChR , AChE
T3736	Olivetol	5-Pentylresorcinol,5-n-Amylresorcinol	Cannabinoid Receptor , P450 , IκB/IKK
	Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an...		Cannabinoid Receptor , P450 , IκB/IKK
TQ0109	Cephaeline dihydrochloride	(-)-Cephaeline dihydrochloride,NSC 32944	P450
	(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM).		P450
TQ0296	N-Nornuciferine		P450
	N-Nornuciferine, an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).		P450
TN1210	2-Hydroxy-1-Methoxyaporphine		P450
	2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.		P450
TN1011	Rhodionin		P450 , AChE
	Rhodionin and rhodionin can inhibit cytochrome P450 2D6 non-competitively with high specificity which could have implications for interactions with co-administered drugs; they can significantly suppress the elevation of ...		P450 , AChE
T3852	Rhodiosin		Antioxidant , AChE
	Rhodiosin is a compound with antioxidant activity.		Antioxidant , AChE