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- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
S-EMCA
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1199796-29-6
- 规格:
10 mM * 1 mL/2 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥3470.0 |
|---|---|---|---|
| 规格: | 2 mg | 产品价格: | ¥2333.0 |
| 规格: | 5 mg | 产品价格: | ¥3500.0 |
| 规格: | 10 mg | 产品价格: | ¥5000.0 |
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INT-777
CAS No. : 1199796-29-6
MCE 国际站:INT-777
产品活性:INT-777是有效的 TGR5 激动剂,EC50 为 0.82 μM。
研究领域:GPCR/G Protein
作用靶点:G protein-coupled Bile Acid Receptor 1
In Vitro: INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity. INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner. INT-777 (10 μM) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations.
In Vivo: INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its chole-hepatic shunt pathway with a ductular absorption and a potent choleretic effect in HF-fed TGR5-Tg male mice. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high-fat feeding in TGR5-Tg mice.
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