Catalog No.
Product Name
Application
Product Information
Citations
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GPR120 agonist
GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209. -
SST4 receptor agonist
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. -
kappa opioid agonist
ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye. -
guanylate cyclase stimulator
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM. -
drug-linker conjugate for ADC
AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2. -
drug-linker conjugate for ADC
AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC. -
hV1a receptor antagonist
Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism. -
angiotensin II receptor antagonist
Pratosartan is a selective angiotensin II receptor antagonist. -
BB1/BB2 antagonist
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. -
5-HT2C receptor-selective agonist
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM. -
triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist. -
OX2R antagonist
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). -
CXCR7 modulator
CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM. -
β-adrenoceptor blocking agent
(±)-Befunolol is a β-adrenoceptor blocking agent. -
PGI2 receptor agonist and vasodilator
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation. -
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.
