Powder: -20°C for 3 years | In solvent: -80°C for 1 year
INT-777(S-EMCA)是有效的 TGR5 激动剂,EC50 为 0.82 μM。 INT-777(S-EMCA)在大鼠蛛网膜下腔出血后通过 TGR3/cAMP/PKA 信号通路抑制 NLRP5-ASC 炎症小体介导的神经炎症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,280 | 现货 | ||
2 mg | ¥ 1,930 | 现货 | ||
5 mg | ¥ 2,890 | 现货 | ||
10 mg | ¥ 4,160 | 现货 | ||
25 mg | ¥ 6,520 | 现货 | ||
50 mg | ¥ 8,790 | 现货 | ||
100 mg | ¥ 11,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,880 | 现货 |
产品描述 | INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway after subarachnoid hemorrhage in rats. |
靶点活性 | TGR5:0.82 μM(EC50) |
体外活性 |
INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner.[2] INT-777 (10 μM) decreased Isc and increased TEER when added to the serosal side of serosal-stripped distal colon segments. The effect of INT-777 on basal secretion was reduced in neuronal-free and TTX-treated muco-submucosal preparations.[3] |
体内活性 |
INT-777 (1 μM/min/kg; orally) is a potent choleretic that prevents activation and subsequent binding of carboxy-CoA, thus favoring its biliary-hepatic shunt pathway with ducts in HF-fed TGR5-Tg males Absorption and strong choleretic effect in mice.[1] INT-777 (30 mg/kg/day; orally) increases energy expenditure and reduces hepatic steatosis and adiposity when fed high fat in TGR5-Tg mice.[2] |
别名 | S-EMCA |
分子量 | 450.65 |
分子式 | C27H46O5 |
CAS No. | 1199796-29-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 50 mg/mL (110.95 mM)
DMSO: 30 mg/mL (66.57 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.219 mL | 11.0951 mL | 22.1902 mL | 55.4754 mL |
5 mM | 0.4438 mL | 2.219 mL | 4.438 mL | 11.0951 mL | |
10 mM | 0.2219 mL | 1.1095 mL | 2.219 mL | 5.5475 mL | |
20 mM | 0.111 mL | 0.5548 mL | 1.1095 mL | 2.7738 mL | |
50 mM | 0.0444 mL | 0.2219 mL | 0.4438 mL | 1.1095 mL | |
Ethanol | 100 mM | 0.0222 mL | 0.111 mL | 0.2219 mL | 0.5548 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
INT-777 1199796-29-6 GPCR/G Protein GPCR19 INT777 INT 777 S-EMCA Inhibitor inhibitor inhibit