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T41003 |
KG5
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|
Raf
,
FLT
,
PDGFR
,
c-Kit
|
|
KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities. |
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T67956 |
Litoxetine
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|
5-HT Receptor
|
|
Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently r... |
|
T22697 |
CS 2100
|
1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid |
S1P Receptor
|
|
CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) is an S1P1 agonist. |
|
T36126 |
TMP-153
|
|
|
|
Acyl-CoA:cholesterol acyltransferase (ACAT) catalyses the esterification of excess cellular cholesterol with fatty acids and is important for intestinal cholesterol absorption, hepatic lipoprotein secretion, and choleste... |
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T4039 |
BIBB 515
|
|
Others
|
|
BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of... |
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T35666 |
PRGL493
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|
Others
|
|
PRGL493 is an inhibitor of long-chain acyl-CoA synthetase 4 (ACSL4).1It inhibits formation of arachidonoyl-CoA (AA-CoA) from arachidonic acid in, as well as the proliferation and migration of, PC3 and MDA-MB-231 cancer c... |
|
T36696 |
DMBA
|
|
|
|
7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzy... |
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T35689 |
MTP 131 acetate
|
|
Others
|
|
MTP 131 is a mitochondria-targeted peptide antioxidant.1,2It localizes to the mitochondria and reducestert-butyl hydroperoxide-induced lipid peroxidation and apoptosis in SH-SY5Y cells when used at concentrations ranging... |
|
T36949 |
Niaprazine
|
|
5-HT Receptor
,
Adrenergic Receptor
,
Histamine Receptor
|
|
Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2].
Niaprazine exhibits a low aff... |
|
T38192 |
Unifiram
|
|
Others
|
|
Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the ra... |
|
T37190 |
L-Allylglycine
|
|
Dehydrogenase
,
GABA Receptor
|
|
L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol/g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol/kg, ... |
|
T38294 |
4-Deoxypyridoxine hydrochloride
|
|
S1P Receptor
|
|
4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhib... |
|
T36520 |
COR659
|
|
Cannabinoid Receptor
,
GABA Receptor
|
|
COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1].
COR659 apparently exerts its effects via a composite mechanism, including positive allosteri... |
|
T24742 |
RS-67333
|
RS67333 |
|
|
RS-67333 is a 5-HT4R partial agonist. It shows efficacy at 0.3 and 1.0 mg/kg, ip. |
|
T61639 |
S1P1 agonist 4
|
|
|
|
S1P1 agonist 4 exhibits enhanced potency with an EC 50 value of less than 0.05 mg/kg and a predicted human half-life (t1/2) of approximately 5 days, indicating a favorable pharmacological profile. |
|
T37114 |
SB 242084 dihydrochloride
|
|
|
|
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242... |
|
T79399 |
E2730
|
|
GABA Receptor
|
|
E2730 is a selective and noncompetitive inhibitor of the gamma-aminobutyric acid (GABA) transporter 1 (GAT1) that exhibits oral availability as well as antiepileptic properties. Its inhibition of GAT1 is dependent on the... |
|
T36543 |
Prostaglandin B2
|
PGB2 |
|
|
Prostaglandin B2 (PGB2) is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the ... |
|
T38209 |
Hodgkinsine
|
|
|
|
Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test i... |
|
T34707 |
SST-02
|
SST 02,SST02 |
|
|
SST-02 is a potent cationic lipid for siRNA-Lipid Nanoparticles. SST-02 possesses a simple chemical structure and is synthesized just in one step. SST-02 showed an ID50 of 0.02 mg/kg in the factor VII (FVII) model. Rats ... |
|
T35439 |
(E)-5-(2-Bromovinyl)uracil
|
|
|
|
(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibl... |
|
T36811 |
UPSEM 817 tartrate
|
|
|
|
Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical ... |
|
T35513 |
13C15-Nivalenol
|
13C15-Nivalenol |
|
|
13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/k... |
|
T36639 |
Donecopride (fumarate hydrate)
|
|
|
|
Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= ... |
|
T79735 |
DHFR-IN-9
|
|
|
|
DHFR-IN-9 (compound 8A), a dihydrofolate reductase (DHFR) inhibitor, impedes purine and thymidylate biosynthesis, pivotal in cell proliferation and growth. It demonstrates potency against methicillin-resistant Staphyloco... |
|
T35517 |
4-deoxy Nivalenol-13C15
|
4-deoxy Nivalenol-13C15 |
|
|
4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It binds to e... |
|
T37391 |
PSEM 308 hydrochloride
|
|
|
|
PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neuro... |
|
T69104 |
SAX-187 hydrochloride
|
|
|
|
SAX-187 hydrochloride is a potent and selective 5-HT6 receptor agonist. SAX-187 hydrochloride possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonis... |
|
T36404 |
PRLX-93936
|
|
|
|
PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1... |
|
T36101 |
Psychotridine
|
|
|
|
Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values ... |
|
T36296 |
BIO5192 hydrate
|
|
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase... |
|
T83665 |
α-Helical CRF (9-41) TFA
|
α-Helical Corticotropin-Releasing Factor (9-41) |
|
|
α-Helical CRF (9-41) is a synthetic peptide antagonist that targets corticotropin-releasing factor (CRF), effectively inhibiting CRF-induced adrenocorticotropic hormone (ACTH) release both in vitro, with isolated rat ant... |
|
T71328 |
Theobromine-d6
|
|
|
|
Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and... |
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T83776 |
Dopamine D3 Receptor Agonist 13a
|
|
|
|
Dopamine D3 receptor agonist 13a selectively targets the dopamine D3 receptor over dopamine D1, D2, and D4 receptors, with affinities (Ki values) of 0.14, 4,600, 2.85, and 756 nM, respectively. It also interacts with ser... |
|
T35783 |
Zearalenone-13C18
|
Zearalenone-13C18 |
|
|
Zearalenone-13C18is intended for use as an internal standard for the quantification of zearalenone by GC- or LC-MS. Zearalenone is a mycotoxin that has been found inFusariumand has estrogenic activities.1It binds to huma... |
|
T37791 |
A-971432
|
|
|
|
A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cel... |
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T83670 |
F1 TFA
|
Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide |
|
|
F1, an anti-inflammatory peptide, incorporates the HIV-1 Tat protein transduction domain linked with a 15-amino acid sequence from residues 46-60 of the inhibitor of NF-κB kinase-interacting peptide (IKIP). It effectivel... |
|
T64553 |
GLP-1(7-37) TFA salt
|
|
|
|
The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine... |
|
T36160 |
8-iso Prostaglandin E2
|
8-iso Prostaglandin E2 |
|
|
8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with ... |
|
T68332 |
AKI-001
|
|
|
|
AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular... |
|
T28884 |
SUN-C5174
|
SUNC-5174 |
|
|
SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in ca... |
|
T36054 |
D13
|
|
|
|
D13 is an acylhydrazone antifungal.1 It is active against C. neoformans in vitro (MIC80 = 0.06 μg/ml). D13 (20 mg/kg per day, p.o.) increases survival in mouse models of C. neoformans, C. albicans, or A. fumigatus infect... |
|
T36629 |
Givinostat
|
|
|
|
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF30... |
|
T83887 |
SLU-10482
|
|
|
|
SLU-10482, an antiparasitic agent, effectively reduces C. parvum parasitic load in HCT-8 cells with an EC50 value of 0.07 µM. It exhibits lower affinity for human ether-a-go-go (hERG; Kd = 43 µM) compared to its counterp... |
|
T37167 |
Reduced Haloperidol
|
|
|
|
Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4... |
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T71300 |
Pentoxifylline-d6
|
|
|
|
Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human er... |
|
T36521 |
Alaproclate (hydrochloride)
|
|
|
|
Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s =... |
|
T36108 |
YW3-56 (hydrochloride) (technical grade)
|
YW3-56 (hydrochloride) (technical grade) |
|
|
YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of ... |
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T83773 |
Prostaglandin E2 Inhibitor 3
|
PGE2 Inhibitor 3 |
|
|
Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO... |
|
T68356 |
AM-3189
|
|
|
|
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displa... |
