- TC-G-1008
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- $32.00
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2026-08-20
- CAS:1621175-65-2
- Purity: 99.54%
- Supply Ability: 10g
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| | GPR39-C3 Basic information |
| Product Name: | GPR39-C3 | | Synonyms: | GPR39-C3;TC-G-1008;N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide;GPR39C3;GPR39 C3;CS-2374;TC-G-1008 (GPR39-C3);Methanesulfonamide, N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-;N-(3-Chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide | | CAS: | 1621175-65-2 | | MF: | C18H19ClN6O2S | | MW: | 418.9 | | EINECS: | | | Product Categories: | | | Mol File: | 1621175-65-2.mol |  |
| | GPR39-C3 Chemical Properties |
| Boiling point | 662.1±65.0 °C(Predicted) | | density | 1.462±0.06 g/cm3(Predicted) | | storage temp. | 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 | | InChI | 1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24) | | InChIKey | DRSZMILOMUPIBJ-UHFFFAOYSA-N | | SMILES | CNC1=NC(C2=CC=CC=N2)=CC(NCC3=C(Cl)C=C(NS(C)(=O)=O)C=C3)=N1 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | GPR39-C3 Usage And Synthesis |
| 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 +4°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 |
| | GPR39-C3 Preparation Products And Raw materials |
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