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Catalog No.
Product Name
Application
Product Information
Product Citation
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S1PR1 modulators
RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases. -
EP2 Agonist
C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM. -
β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
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5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
prostaglandin EP4 receptor antagonist
Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
CCK-2 receptor antagonist
Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
dopaminergic stabilizer
ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission. -
dopamine D2 receptor agonist
UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.- Anika Mann, .et al. , Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
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GLP-1 receptor agonist
Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist. -
V1b receptor antagonist
Vasopressin antagonist, Orally available and selective V1b receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over hV1a, hV2, and hOT). -
REV-ERBα/β agonist
SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM. - Prostaglandin F2α is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
- Michel R Corboz, .et al. , Prostaglandins Other Lipid Mediat, 2020, Oct 1;152:106486 PMID: 33011365
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β-adrenoceptor agonist
Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist. -
LPA1 antagonist
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. -
GLP-1 agonist
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).- Tito Borner, .et al. , Cell Rep, 2020, Jun 16;31(11):107768 PMID: 32553160
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MC1R and MC5R antagonist
JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells. -
Endogenous galanin receptor agonist
Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects - Glucagon-Like Peptide 1 (7-36) Amide is a potent glucose-dependent insulinotropic peptide produced by post-translational processing of proglucagon in intestinal L-cells.
- Ying Zhou, .et al. , Adv Biol (Weinh), 2022, Nov 14 PMID: 36373695
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NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
CGRP receptor antagonist
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
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CRF-1 antagonist
Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. -
DP1 receptor antagonist
Asapiprant, also known as S-555739, is a the potent and selective DP1 receptor antagonist. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. -
H4 receptor antagonist
JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM. -
5-HT(2A) receptor agonist
Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis. -
Dopamine D1/2 receptor antagonist
Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function. -
serotonin uptake inhibitor
Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression. -
5-HT3 receptor antagonist
Dolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. -
histamine H1 receptor antagonist
Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. This medication is an antihistamine, prescribed for allergic conjunctivitis. -
Histamine H2-receptor antagonist
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. -
beta-adrenergic agonist
Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent. -
β-adrenergic receptor antagonist
Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma. -
Somatostatin Receptor agonist
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). -
CCKA receptor antagonist
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
