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INT-777

SKU: orb1709405

Description

INT-777 (S-EMCA) is a potent TGR5 receptor agonist exhibiting an EC50 of 0.82 μM. It has been shown to suppress neuroinflammation by inhibiting the NLRP3-ASC inflammasome via the TGR5/cAMP/PKA pathway in rat models of subarachnoid hemorrhage, highlighting its utility in neuroscience and inflammation research.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1199796-29-6
MW450.65
Purity99.89% (May vary between batches)
FormulaC27H46O5
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
TargetGPCR19
SolubilityDMSO:30 mg/mL (66.57 mM);Ethanol:50 mg/mL (110.95 mM)

Bioactivity

Target IC50
COS-1 cells:> 100 μM (EC50)|NCI-H716 cells:0.82 μM (EC50)|HEK293 cells:0.36 μM (EC50)|CHO cells:3.44 μM (EC50)|TGR5:0.82 μM (EC50)
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. INT-777 (30 mg/kg/day; orally) increases energy expenditure and reduces hepatic steatosis and adiposity in high-fat-fed TGR5-Tg mice.
In Vitro
INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner. 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

INT 777, INT777, INT-777, S-EMCA, TGR5

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Quality Guarantee

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Protocol Information

INT-777 (orb1709405)

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% DMSO +
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% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 2,340.00
5 mg
¥ 5,070.00
1 ml x 10 mM (in DMSO)
¥ 5,590.00
10 mg
¥ 7,020.00
25 mg
¥ 11,440.00
50 mg
¥ 15,600.00
100 mg
¥ 20,800.00
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