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S82300

INT-777

源叶(MedMol) 98%
  • 英文名:
  • INT-777
  • 别名:
  • INT 777; (2S,4R)-4-[(3R,5S,6R,7R,8R,9S,10S,12S,13R,14S,17R)-6-ethyl-3,7,12-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methylpentano
  • CAS号:
  • 1199796-29-6
  • 分子式:
  • C27H46O5
  • 分子量:
  • 450.6512
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S82300-5mg 98% ¥2900.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82300-10mg 98% ¥4100.00元 预计交期:2-3天 - - - EA 加入购物车
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参考文献

质检证书(COA)

摩尔浓度计算器

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  • 提示:详情请下载说明书。
  • 产品描述: INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM
  • 靶点: EC50: 0.82 μM (TGR5);GPCR19
  • 体外研究:
    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
  • 体内研究:
    INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its cholehepatic 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
  • 参考文献:
    1. Pellicciari R, et al. Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem. 2009 Dec 24;52(24):7958-61. 2. Thomas C, et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009 Sep;10(3):167-77. 3. Duboc H, et al.Reduction of epithelial secretion in male rat distal colonic mucosa by bile acid receptor TGR5 agonist, INT-777: role of submucosal neurons. Neurogastroenterol Motil. 2016 Jun 3. doi: 10.1111/nmo. 4. Baiqiang Li, et al. INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis. Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44.
  • 溶解性: Soluble  in  DMSO、Ethanol
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.219 ml 11.095 ml 22.19 ml
    5 mM 0.444 ml 2.219 ml 4.438 ml
    10 mM 0.222 ml 1.11 ml 2.219 ml
    50 mM 0.044 ml 0.222 ml 0.444 ml
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