GPR39-C3 MedChemExpress (MCE)

Product Name	TC-G-1008
Synonyms	GPR39C3 CS-2374 GPR39 C3 GPR39-C3 TC-G-1008 16211175-65-2 TC-G-1008 (GPR39-C3) Synonyms GPR39C3 CS-2374 GPR39 C3 GPR39-C3 TC-G-1008 16211175-65-2 TC-G-1008 (GPR39-C3) N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide N-(3-Chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide Methanesulfonamide, N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-
CAS	1621175-65-2
EINECS
Chemical Formula	C18H19ClN6O2S
Molecular Weight	418.9
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg
Price	Email to quote
Descriptions	TC-G-1008 TC-G-1008 MedChemExpress (MCE) HY-103007 1621175-65-2 GPR39-C3 99.61% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions TC-G-1008 TC-G-1008 MedChemExpress (MCE) HY-103007 1621175-65-2 GPR39-C3 99.61% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively. TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound[2]. Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively[1]. Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1]. HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white, 384-well plates (4000 cells/well) in the growth medium overnight at 37°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TC-G-1008) or vehicle control (DMSO), the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37°C. Then, the compound solution is removed and washed twice with PBS containing 0.1% BSA. For measurement of intracellular cAMP, the cells are stimulated with drugs in stimulation buffer for 30 min at 37°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2]. IC50: 0.4 nM (GPR39), 0.8 nM (GPR39)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Peukert S, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4 5(10):1114-8. [Content Brief] [2]. Shimizu Y, et al. Rho kinase-dependent desensitization of GPR39 a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15 140:105-114. [Content Brief]
Last Update	2025-04-01 14:45:47

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