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Catalog No.
Product Name
Application
Product Information
Citations
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5-HT3 receptor antagonist
Dolasetron mesylate is a selective 5-HT3 receptor antagonist. -
Histamine 1 receptor antagonist
Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis. -
hemagglutinin (HA)-receptor antagonist
Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. -
LTR antagonist
Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. -
5-HT1A receptor antagonist
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. -
S1P antagonist
Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant. -
Serotonergic receptor antagonist
(Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1. -
histamine H1-receptor antagonist
Diazoline is a histamine H1-receptor antagonist. -
histamine H1 antagonist
Chlorcyclizine hydrochloride is a histamine H1 antagonist. -
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. -
Dopamine D2 antagonist
Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic. -
CCK antagonist
Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist. -
Histamine H1 antagonist
Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. -
5-HT receptor /dopamine receptors antagonist
Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors. -
β-adrenergic receptor antagonist
Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity. -
dopamine D2 receptor antagonist
Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic. -
α2 adrenoceptor antagonist
Piperoxan hydrochloride is an α2 adrenoceptor antagonist. -
Sigma-1 receptor antagonist
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (??1) receptor antagonist with a Ki of 1.14 nM. -
sigma 1 receptor antagonist
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, 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). -
κ opioid receptor antagonist
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. -
EPAC2 antagonist
ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 ?M. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.- Yuri A Blednov, .et al. , Neuropharmacology, 2024, Jun 13:257:110035 PMID: 38876310
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neuropeptide Y1 receptor antagonist
BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over ??1, α1, Y2, Y4 and Y5 receptors respectively. -
SSTR5 antagonist
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM). -
CB1 antagonist
CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM. -
PAR4 antagonist
UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). -
μ-opioid receptor antagonist
GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. -
NOP receptor antagonist
LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models. -
mGlu2/3 antagonist
LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. -
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. -
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. -
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). -
EP4 receptor antagonist
BAY-1316957 is a highly potent and selective EP4 receptor antagonist with an IC50 of 15.3 nM. Good oral bioavailability.
