Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
mGluR antagonist
SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype. -
5-HT4 Receptor Antagonist
SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist. -
5-HT3 receptor antagonist
Tropanserin acts as a potent and selective 5-HT3 receptor antagonist. -
adrenergic alpha-2 receptor agonist
Medetomidine Hydrochloride is an adrenergic alpha-2 receptor agonist, which is used in veterinary medicine for its analgesic and sedative properties. -
ETA antagonist
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA). -
5-HT1A/1B and 5-HT2C agonist
RU 24969 succinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.
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Dopamine receptor agonist
Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist. - Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
- Flibanserin is a new drug being investigated for the prevention of HSDD in woman.
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norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor -
prostacyclin receptor agonist
NS-304 is a selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors). -
Smoothened inhibitor
PF-04449913 is a potent and orally bioavailable inhibitor of smoothened. -
α2 adrenergic receptor antagonist
Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant. - Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
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A2A receptor antagonist
Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease.
