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Catalog No.
Product Name
Application
Product Information
Product Citation
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5-HT Receptor antagonist
Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist. -
Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
Dopamine Receptor antagonist
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. -
neurokinin-1 receptor antagonist
Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.
- Maya Tokumoto, .et al. , Connect Tissue Res, 2022, Jul 20;1-11 PMID: 35856812
- Kodji X, .et al. , FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150
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H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production. -
Histamine Receptor antagonis
Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine. -
Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. -
S1P Receptor antagonist
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.- Tina Sepasi, .et al. , Int J Pharm, 2023, Apr 5;636:122815 PMID: 36907279
- Tina Sepasi, .et al. , BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. , Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. , Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. , Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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PAFR antagonist
Ginkgolide B (BN 52021) is a PAFR antagonist with IC50 of 3.6 μM. -
5-HT3 receptor antagonist
Granisetron HCl is a serotonin 5-HT3 receptor antagonist -
AT1 antagonist
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. -
5-HT2A serotonin receptor antagonist
Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. -
LPA Receptor Antagonist
Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3 and exhibits Ki values of 0.34, 6.5, and 0.93 μM for the human LPA1, LPA2, and LPA3 receptors, respectively.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. , PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. , Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. , Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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Smo Antagonist
LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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5-HT2/5-HT1 antagonist
Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant. -
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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5-HT1A and α1-adrenergic receptor antagonist
Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. -
5-HT Receptors/D2 dopamine receptor antagonist
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. -
5-HT Receptors antagonist
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy. -
Dopamine Receptor antagonist
Paliperidone(Invega) is an atypical antipsychotic.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
5-HT2C receptor antagonist
Puerarin is one of several known isoflavones. Puerarin is a 5-HT2C receptor and benzodiazepine site antagonist. Puerarin is being investigated as a self-microemulsifying drug delivery system.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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α1-adrenoceptor antagonist
Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). -
Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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LTD4 receptor antagonist
Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist. -
ETA-receptor Antagonist
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
SMO Antagonist
LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein. -
neurokinin-1 receptor antagonist
Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist. -
Opioid Receptor antagonist
JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.- Lihao Gu, .et al. , Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. , Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. -
AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
CaSR antagonist
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. -
5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
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5HT1A antagonist
WAY-100635 was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor.
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5-HT3 antagonist
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. -
CGRP receptor antagonist
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. -
EndothelinA receptor antagonist
Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).- Naoki Dohi, .et al. , PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. , World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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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 -
Endothelin antagonist
Avosentan (SPP301) is a potent and highly selective ETA receptor blocker. -
Serotonin 5HT3-receptor antagonist
Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. -
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
