Catalog No.
Product Name
Application
Product Information
Product Citation
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Adrenergic Receptor agonist
Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline. -
Adrenoceptors agonist
UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist. -
Adrenergic Receptor agonist
Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR. -
Dual orexin receptor antagonist
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).- Tung-Yen Lee, .et al. , Front Psychiatry, 2023, Jun 29;14:1196994 PMID: 37457782
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Histamine H4 receptor antagonist
A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). - Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.
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serotonin uptake inhibitor
Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively). -
GPR40/FFA1 agonist
AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist. -
Kainate receptor agonist
Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms. -
prostaglandin F2α analog
Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α. -
5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors). -
Adenosine A2A receptor antagonist
Preladenant is a potent and selective antagonist at the adenosine A2A receptor. -
D2 dopamine partial agonist
Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). -
adrenergic receptor antagonist
Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro. -
SMO agonist
SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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2A-AR adrenergic agonist
Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand. -
EDG-1 (S1P1) agonist
CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM). -
histamine H3 receptor agonist
Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively). -
human 5'-methylthioadenosine phosphorylase inhibitor
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. -
β3 adrenergic agonist
CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice. -
5HT2A antagonist
Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors. -
guanylate cyclase (sGC) stimulator
Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay. -
CCK-2 receptor antagonist
Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
dopamine β-hydroxylase (DBH) inhibitor
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. -
β3-adrenergic receptors agonist
BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity. -
NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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D2 dopamine receptor antagonist
L-741626 is a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
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dopamine D2 receptor agonist
Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism. -
CCK antagonist
Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini. -
somatostatin receptor 2 antagonist
CYN-154806 is a potent selective somatostatin receptor 2 (sst2) antagonist. -
TGR5(GPCR19) agonist
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). -
adenosine A2B receptors antagonist
CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. -
dual antagonist of TP/DP2
BAY-u 3405 is an approved human medication for the treatment of allergic rhinitis that has documented activity as an antagonist of the thromboxane receptor (TP receptor). -
Oxytocin antagonist
PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
