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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $139 | In Stock | |
2 mg | $198 | In Stock | |
5 mg | $347 | In Stock | |
10 mg | $497 | In Stock | |
25 mg | $838 | In Stock | |
50 mg | $1,160 | In Stock | |
100 mg | $1,560 | In Stock | |
1 mL x 10 mM (in DMSO) | $382 | In Stock |
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 binding of carboxy-CoA, favoring its biliary-hepatic shunt pathway in HF-fed TGR5-Tg males, and shows absorption and strong choleretic effect in mice.[1] INT-777 (30 mg/kg/day; orally) increases energy expenditure and reduces hepatic steatosis and adiposity in high-fat-fed TGR5-Tg mice.[2] |
Alias | S-EMCA |
Molecular Weight | 450.65 |
Formula | C27H46O5 |
Cas No. | 1199796-29-6 |
Smiles | [H][C@@]12CC[C@H]([C@H](C)C[C@H](C)C(O)=O)[C@@]1(C)[C@@H](O)C[C@@]1([H])[C@@]2([H])[C@H](O)[C@H](CC)[C@]2([H])C[C@H](O)CC[C@]12C |
Relative Density. | 1.128 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 50 mg/mL (110.95 mM) DMSO: 30 mg/mL (66.57 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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