Catalog No.
Product Name
Application
Product Information
Citations
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δ-opioid receptor modulator
BMS-986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor. -
δ-opioid receptor modulator
BMS-986187 is a potent and selective positive allosteric modulator (PAM) of the δ-opioid receptor and a G-protein-biased allosteric agonist. -
bovine tubulin oxidation inhibitor
Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor. -
histamine H1 receptor antagonist
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. -
antiplatelet activities
6-Methoxydihydroavicine is an alkaloid isolated from Zanthoxylum integrifoliolum. 6-Methoxydihydroavicine has antiplatelet activities and inhibits AA-, collagen- and PAF-induced platelet aggregation in vitro. -
A1 adenosine receptor agonist
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. - SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties.
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β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol 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.
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histamine H3R antagonist/inverse agonist
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. -
5-HT3 receptor antagonist
5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system. -
CXCR4 antagonist
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM. -
analgesic agent
Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. -
leukotriene B4 receptor antagonist
Etalocib, also known as LY293111 and VML295, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5'-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor. -
melanocortin receptor (MR) agonist
AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. -
GLP-1R agonist
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R) -
5-HT4 receptor partial agonist
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. -
5-HT7 receptor antagonist
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. -
5-HT receptor agonist
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). - Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
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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. -
mGlu1 receptors modulator
Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. -
mGluR agonist
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively. -
guanylate cyclase stimulator
Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator. -
EP2 receptor agonist
Taprenepag isopropyl is a highly selective EP2 receptor agonist. -
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.
