Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | 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 |
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 |
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.
You can also refer to dose conversion for different animals. More
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INT-777 1199796-29-6 GPCR/G Protein GPCR19 INT777 INT 777 S-EMCA inhibitor inhibit