Catalog No.
Product Name
Application
Product Information
Product Citation
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5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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adrenergic agonist
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. - Prostaglandin E1 (PGE1) is the theoretical cyclooxygenase metabolite of dihomo-γ-linolenic acid (DGLA), but it is virtually undetectable in the plasma of normal humans or other animals. The IC50 of PGE1 for the inhibition of ADP-induced human platelet aggregation is 40 nM.
- Hang Dong, .et al. , Int J Nanomedicine, 2023, 18: 3577-3593 PMID: 37409026
- Baharak Bahmani, .et al. , Nat Commun, 2021, Mar 31;12(1):1999 PMID: 33790276
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D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. -
β2-adrenergic receptor
Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties. -
alpha2-adrenoceptor agonist
Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist - Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
- Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
- Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
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Leukotriene receptor antagonist
Pranlukast is a selective cysteinyl leukotriene receptor antagonist. - Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
- Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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CB receptor agonist
WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.- Greish K, .et al. , J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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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. -
CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
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GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
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. -
mGlu4 receptor modulator
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. -
lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. -
PAR4 antagonist
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. -
PAF antagonist
Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo. -
5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. -
5-HT4 receptor antagonist
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. -
5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
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.