Catalog No.
Product Name
Application
Product Information
Citations
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EP4 receptor antagonist
BAY-1316957 is a highly potent and selective EP4 receptor antagonist with an IC50 of 15.3 nM. Good oral bioavailability. - Thrombin Receptor Activator for Peptide 5 (TRAP-5), coagulation factor II (thrombin) receptor is a G protein-coupled receptor involved in the regulation of thrombotic response.
- Big Endothelin-1 (1–38), human, is the biologically inactive precursor of endothelin-1 (ET-1), a potent endogenous vasoconstrictive peptide. Upon enzymatic cleavage by endothelin-converting enzymes (ECEs), Big Endothelin-1 is processed into the active ET-1 form, which plays a critical role in the regulation of vascular tone and blood pressure. This peptide is widely used as a research tool for investigating endothelin signaling pathways, cardiovascular physiology, and related pathophysiological processes.
- Corticotropin Releasing Factor, bovine, neurotransmitter and CRF receptor antagonist.
- Endothelin-2, human, endogenous peptide found predominately in the kidney and intestine. Displays similar selectivity for ETA and ETB endothelin receptors.
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α1 receptor antagonist
Tamsulosin hydrochloride is a selective α1 receptor antagonist and a medicine which is used in benign prostatic hyperplasia. -
ET-A and ET-B antagonist
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. -
β2-adrenoceptor agonist
Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD). -
5HT3-receptor antagonist
Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. -
μ-opioid receptor agonist
Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
μ-opioid receptor agonist
Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
CXCR4 antagonist
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. -
GHSR stimulator
Anamorelin fumarate is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia. -
adrenergic receptor/5-HT receptor inhibitor
Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. -
Endothelin antagonist receptor
Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer. -
H3 receptor antagonist
Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
H3 receptor antagonist
Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
α-adrenergic receptor agonist
Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension. -
D3/D2 Dopamine Receptor Antagonist
Cariprazine hydrochloride is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors. -
H1-receptor antagonist
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. -
H1 histamine receptor antagonist
Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. -
dopamine agonist
Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist. -
H2-receptor antagonist
Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. - GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
- GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
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5-HT3 antagonist
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. -
α2A-adrenoceptor agonist
Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. -
μ-opioid antagonist
Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation. -
Dopamine Receptor antagonist
Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic. -
mGlu5 antagonist
MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively. -
Dopamine reuptake inhibitor
Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam. -
Nonimidazole inverse agonist
Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). -
Nonimidazole inverse agonist
Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). - Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
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D2 receptor agonist
rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. -
CXCL8 receptor inhibitor
Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
