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INT-777

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Catalog No. T11662LCas No. 1199796-29-6
Alias 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.

INT-777

INT-777

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Purity: 99.78%
Catalog No. T11662LAlias S-EMCACas No. 1199796-29-6
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$139In StockIn Stock
5 mg$347In StockIn Stock
10 mg$496In StockIn Stock
25 mg$795In StockIn Stock
50 mg$1,110-In Stock
100 mg$1,550-In Stock
1 mL x 10 mM (in DMSO)$381In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Batch Information

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Purity:99.78%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
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]
SynonymsS-EMCA
Chemical Properties
Molecular Weight450.65
FormulaC27H46O5
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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.2190 mL11.0951 mL22.1902 mL110.9508 mL
5 mM0.4438 mL2.2190 mL4.4380 mL22.1902 mL
10 mM0.2219 mL1.1095 mL2.2190 mL11.0951 mL
20 mM0.1110 mL0.5548 mL1.1095 mL5.5475 mL
50 mM0.0444 mL0.2219 mL0.4438 mL2.2190 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0222 mL0.1110 mL0.2219 mL1.1095 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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