CS-2374

CS-2374化学性质

沸点 :662.1±65.0 °C(Predicted)
密度 :1.462±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :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)
形态 :A crystalline solid
酸度系数(pKa) :7.43±0.10(Predicted)
颜色 :White to off-white

CS-2374性质、用途与生产工艺

生物活性 TC-G-1008（GPR39-C3）是一种有效的、口服活性的 G-protein coupled receptor 39 (GPR39)(zinc receptor) 激动剂，对大鼠受体和人类受体的EC50值分别为0.4 nM 和0.8 nM。
靶点
Target Value
rGPR39
(Cell-free assay) 0.4 nM(EC50)
hGPR39
(Cell-free assay) 0.8 nM(EC50)
体外研究

TC-G-1008 shows selectivity over a panel of kinases (IC ₅₀ s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC ₅₀ s>30 μM). 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.
体内研究

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.

CS-2374上下游产品信息

上游原料

下游产品

CS-2374 试剂级价格

CS-2374生产厂家