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Catalog No.
Product Name
Application
Product Information
Citations
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5-HT6 receptor antagonist
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). -
β adrenergic receptor antagonist
Spirendolol is a β adrenergic receptor antagonist. -
5-HT2A/α1-adrenergic receptor antagonist
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. -
5-HT2A/dopamine D2 antagonist
Abaperidone is a potent antagonist of 5-HT2A?receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM. -
AA3R antagonist
Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist. -
LPA1 antagonist
BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. -
dopamine autoreceptor antagonist
CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist. -
OX2R antagonist
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. -
ostsynaptic alpha adrenergic receptor antagonist
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist. -
CXCR2 receptor antagonist
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor. -
δ opioid receptor antagonist
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM. -
mGlu1 receptor antagonist
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM. -
glucagon receptor antagonist
PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs. -
glucagon receptor antagonist
Adomeglivant is a potent and selective glucagon receptor antagonist that is used in clinical trial for type 2 diabetes mellitus. -
μ-opioid receptor (MOR) antagonist
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. -
5-HT7 receptor antagonist
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively. -
dopamine D2 receptor antagonist
Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor. -
glucagon-like peptide 1 receptor antagonist
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM. -
triple tachykinin receptor antagonist
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. -
NK3R antagonist
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. -
PAF antagonist
Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action. -
5-HT1B receptor antagonist
SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity. -
5-HT2/sigma 2 receptor antagonist
Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia. -
neurokinin receptors antagonist
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS). -
dual dopamine and serotonin receptor antagonist
Deschloroclozapine is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively. -
angiotensin II receptor type 1 antagonist
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
