Catalog No.
Product Name
Application
Product Information
Product Citation
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CGRP receptor antagonist
BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect. -
NK1 receptor antagonist
Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. -
tachykinin NK2 receptor antagonist
Ibodutant is a tachykinin NK2 receptor antagonist for the treatment of Irritable Bowel Syndrome with diarrhoea (IBS-D) -
Oxytocin Receptor Antagonist
Retosiban (GSK-221,149-A) is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptor antagonist with >1400-fold selectivity[3] over the related vasopressin receptors -
ultra-long-acting β??? adrenoreceptor agonist
Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05. -
dopamine uptake inhibitor
GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM). -
D2 receptor antagonist
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms. -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. -
NK1R antagonist
Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. -
Orexin receptor antagonist
MK6096, also known as filorexant, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes. -
Sigma-1 antagonist
BD-1047 2HBr is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. -
angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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Smoothened inhibitor
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
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β2 adrenergic antagonist
ICI 118551 hydrochloride is a selective β2 adrenergic antagonist. -
human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20
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5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. -
A1 adenosine receptor agonist
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. - Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
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guanylate cyclase activator
(4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued. -
PAF receptor antagonist
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor. -
Adrenoceptors antagonist
BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration. - Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
- Clenbuterol Hydrochloride is a sympathomimetic β2-adrenoceptor agonist that has been used as a bronchodilator in the treatment of pulmonary diseases such as asthma. At higher doses, clenbuterol acts as an anabolic steroid, favoring skeletal muscle protein synthesis at the expense of fat deposition.
- Younian Xu, .et al. , J Inflamm Res, 2022, Jan 14;15:295-309 PMID: 35058704
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Adrenergic α1 Receptor Antagonist
HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes. -
α2- adrenoceptor antagonist / I2 imidazoline receptor agonist
Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively). -
imidazoline receptor 1 agonist
Moxonidine hydrochloride is a centrally acting antihypertensive agent. -
5-HT1A receptor antagonist
NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. - Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
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α-Adrenergic blocker
Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker. -
norepinephrine (NE) transporter inhibitor
Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus. -
α2-adrenergic receptor antagonist
Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM). -
Adrenoceptors antagonist
S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker. -
β-adrenergic blocker
S(-)-Propranolol Hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. -
Adrenoceptors antagonist
(S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR. -
Adrenoceptors antagonist
SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
