Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3].
Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor[1].
GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
Pheniramine Maleate ia an antihistamine and vasoconstrictor.
INT-777 (R-enantiomer) is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.
CCG-203971 is a second-generation RhoA/myocardin-related transcription factor A (MRTF-A) inhibitor. CCG-203971 potently targets RhoA/C-activated serum response element (SRE)-luciferase (IC50=6.2 μM).
AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.
Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research[1][2].
K-Ras G12C-IN-2 is a novel and irreversible inhibitor of G12C mutant K-Ras protein.
Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation[1][2].
Adrenotensin (human) (Pro-ADM-153-185 (human)) is a 153-185 fragment of precursor peptide of Adrenomedullin. Adrenomedullin (ADM) is a 52-amino acid multifunctional peptide, which belongs to the CGRP superfamily of vasoactive peptide hormones[1].
Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca2+]i due to Ca2+ release from intracellular stores[1][2].
Treprostinil palmitil (TP) is the prodrug of DP1 and EP2 agonist, Treprostinil (UT-15), whose EC50 values were 0.6 and 6.2 nM, respectively. Treprostinil palmitil is a pure prodrug and possesses no inherent binding to G-protein coupled receptors including prostanoid receptors[1][2].
Neuropeptide Y5 receptor ligand-1 (compound 54), a carbazole derivative, is a potent neuropeptide Y5 (NPY-5) receptor antagonist[1].
mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively[1].
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM)[1].
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1].
11-Deoxy Prostaglandin E2 is a selective agonist of EP4 with an EC50 of 0.66 nM. 11-Deoxy Prostaglandin E2 is an analog of prostaglandin E2. 11-Deoxy Prostaglandin E2 can be used in study bone healing, heart failure, and other receptor associated conditions[1][2].
Trimethobenzamide hydrochloride is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway. Thrombosis Discontinued
VUF 8430 (dihydrobromide) is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM[1].
U66858 is a potent inhibitor of LTB4 production in human whole blood. U66858 also exhibits significant inhibition of lipoxygenase and TXB2 release.
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research[1][2].
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis. The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form. From Wikipedia.
VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration[1].
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain[1].
Antazoline is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect[1][2][3].