47 products were found matching "K04284"!

An antagonist of GHS-Ra (Ki = 0.017 µM), is selective for GHS-Ra over the motilin receptor (Ki = 6 µM) and a panel of 30 receptors and enzymes (Kis = > 10 µM), prevents ghrelin-induced decreases in insulin secretion in glucose-stimulated isolated rat pancreatic islets at concentration of 1 µM, increases plasma...

Recombinant CHO-K1 cells stably overexpress human growth hormone secretagogue receptor (GHSR) on the surface and contain high levels of G protein Galphaq to couple with the receptor in downstream signaling pathways.

Hexarelin is a synthetic hexapeptide agonist of the growth hormone secretagogue receptor (GHS-R). It selectively binds to GHS-R over CD36 (IC50s = 15.9 and 2,080 nM, respectively). Hexarelin (300 µg/kg, s.c.) increases plasma growth hormone levels in neonatal rats. It also improves left ventricular function and...

Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. At 80 µg/kg, JMV3002 inhibits...

GHRP-6 is a synthetic growth hormone (GH) secretagogue and an agonist of the GH secretagogue receptor (GHS-R), which is also known as the ghrelin receptor. It inhibits binding of the GHS-R agonist MK-0677 (ibutamoren, Cay-18003) to COS-7 cell membranes expressing human GHS-R type Ia (Ki = 1.9 nM) and binding of...

PF-05190457 is an inverse agonist of the growth hormone secretagogue receptor (GHS-R), which is also known as the ghrelin receptor. It selectively binds to GHS-R (Ki = 4.37 nM) over M2 muscarinic acetylcholine receptors (mAChRs, Ki = 1,950 nM) and the serotonin (5-HT) receptor subtype 5-HT2B (IC50 = 3,700 nM)....

Description: PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36). Target: GHSR. Smiles: Cc1cn2cc(CC(=O)N3CCC4(CN(C4)[C@@H]4CCc5cc(ccc45)-c4cc(C)ncn4)CC3)nc2s1. References: Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor...

Protein function: Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine). [The UniProt...

Anamorelin is a small molecule agonist of the growth hormone (GH) secretagogue receptor 1a (GHS-R1a) and a mimetic of ghrelin (Cay-15072, Cay-24458, Ki = 0.7 nM). It induces calcium mobilization in CHO cells expressing rat GHS-R1a in a concentration-dependent manner and GH release from rat pituitary cells (EC50 =...

Ghrelin is an endogenous ligand for the growth hormone (GH) secretagogue receptor (GHSR). Ibutamoren is an orally-active, non-peptidic agonist of GHSR (Kd = 0.4 nM) and, as a result, is a GH secretagogue. It elevates GH in dogs after oral doses as low as 0.125 mg/kg, without significantly changing plasma levels of...

Capromorelin is a growth hormone (GH) secretagogue and an agonist of GH secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor. It stimulates GH release from primary rat pituitary cells with an EC50 value of 3 nM. Capromorelin (0.3, 3, and 30 nM) stimulates intracellular calcium mobilization...