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INT-777

Catalog No. T11662L   CAS 1199796-29-6
Synonyms: S-EMCA

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.

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INT-777 Chemical Structure
INT-777, CAS 1199796-29-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 139.00
2 mg In stock $ 198.00
5 mg In stock $ 347.00
10 mg In stock $ 497.00
25 mg In stock $ 838.00
50 mg In stock $ 1,160.00
100 mg In stock $ 1,560.00
1 mL * 10 mM (in DMSO) In stock $ 382.00
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Purity: 99.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 TGR5:0.82 μM(EC50)
In vitro 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]
In vivo 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]
Synonyms S-EMCA
Molecular Weight 450.65
Formula C27H46O5
CAS No. 1199796-29-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 50 mg/mL (110.95 mM)

DMSO: 30 mg/mL (66.57 mM), sonification is recommended.

TargetMolReferences and Literature

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. 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.

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Keywords

INT-777 1199796-29-6 GPCR/G Protein GPCR19 INT777 INT 777 S-EMCA inhibitor inhibit

 

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