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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $139 | In Stock | In Stock | |
| 5 mg | $347 | In Stock | In Stock | |
| 10 mg | $496 | In Stock | In Stock | |
| 25 mg | $795 | In Stock | In Stock | |
| 50 mg | $1,110 | - | In Stock | |
| 100 mg | $1,550 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $381 | In Stock | 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), CHO cells:3.44 μM (EC50), COS-1 cells:> 100 μM (EC50), HEK293 cells:0.36 μM (EC50), NCI-H716 cells: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] |
| Synonyms | 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 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 50 mg/mL (110.95 mM), Sonication is recommended. DMSO: 30 mg/mL (66.57 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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