| Identification | Back Directory | [Name]
GPR39-C3 | [CAS]
1621175-65-2 | [Synonyms]
CS-2374
GPR39-C3
TC-G-1008
GPR39C3;GPR39 C3
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]- | [Molecular Formula]
C18H19ClN6O2S | [MDL Number]
MFCD30182283 | [MOL File]
1621175-65-2.mol | [Molecular Weight]
418.9 |
| Chemical Properties | Back Directory | [Boiling point ]
662.1±65.0 °C(Predicted) | [density ]
1.462±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:63.97(Max Conc. mg/mL);152.72(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:5):0.16(Max Conc. mg/mL);0.38(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.77(Max Conc. mM) | [form ]
A crystalline solid | [pka]
7.43±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively. It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; ) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor. | [Uses]
TC-G 1008 is the first potent, selective, and orally bioavailable GPR39 agonist. | [in vivo]
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]. | [storage]
Store at -20°C | [References]
[1] STEFAN PEUKERT*. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists[J]. ACS Medicinal Chemistry Letters, 2014, 5 10: 1114-1118. DOI: 10.1021/ml500240d |
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| Company Name: |
Twochem Co.Ltd.
|
| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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