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Catalog No.
Product Name
Application
Product Information
Product Citation
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CGRP Receptor antagonist
MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.- Marlene Dallmayer, .et al. , bioRxiv, 2018, 2018
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dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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Opioid Receptor agonist
ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM. -
Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). -
H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. -
CGRP receptor antagonist
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. -
Opioid antagonist
Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract. -
D2 receptor antagonist
Adoprazine is part of the Antidepressant Agent group -
β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. -
CXCR4 antagonist
AMD 070 is a CXCR4 chemokine receptor antagonist.- Uchida D, .et al. , Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. , BMC Cancer, 2016, 16: 305 PMID: 27175473
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mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. -
KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. -
DP1 inhibitor
Laropiprant is used in combination with niacin to reduce blood cholesterol. Laropiprant acts as a DP1 antagonist, reducing the vasodilation. -
EP4 antagonist
MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. -
EP4 antagonist
ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer. - Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
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A2a receptor antagonist
SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders. -
5-HT6 receptor antagonist
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. -
LTD4 receptor antagonist
Verlukast (MK-0679) is a potent leukotriene D4 antagonist -
Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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CaSR agonist
Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid. - Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
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DAT and SLC6A2 inhibitor
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. -
CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. - YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM)
- Lin D, .et al. , Endocrinology. , 2014, 155(7):2355-62 PMID: 24735326
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mGlu4 receptors modulator
VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells. -
MCH-1 antagonist
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM. -
Dopamine receptor antagonist
cis-(Z)-Flupentixol dihydrochloride is a dopamine receptor antagonist, antipsychotic, neuroleptic agent. -
CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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Sigma-2 receptor agonist
Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. -
OX Antagonist
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. -
opioid κ-selective agonist
Nalfurafine hydrochloride is a kappa-opioid receptor agonist- Lin Tian, .et al. , Research Square, 2023, May 30
- Alexander R French, .et al. , Pharmacol Biochem Behav, 2022, May;216:173377 PMID: 35364122
- Wen-Wen Zhang, .et al. , JCI Insight, 2022, Feb 8;7(3):e153191 PMID: 34914639
- A Dunn, .et al. , Psychopharmacology (Berl), 2020, May 20 PMID: 32435819
- Dunn AD, .et al. , ACS Chem Neurosci, 2019, Aug 21;10(8):3590-3600 PMID: 31313902
- Anika Mann, .et al. , Sci Signal, 2019, Mar 26;12(574). pii: eaau8072 PMID: 30914485
- Snyder LM, .et al. , Neuron, 2018, Sep 19;99(6):1274-1288.e6 PMID: 30236284
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D2 receptor antagonist
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7). -
CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
Adenosine receptor inhibitor
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor
