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INT-777

Name: INT-777
Brand: TargetMol
SKU: T11662L
Price: 139 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: S-EMCA) Copy Product Info

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Synonyms: S-EMCA

Catalog No. T11662L Copy Product Info

Purity: 99.78%

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INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.

Cas No. 1199796-29-6

Pack Size	Price	USA Stock	Global Stock
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

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.78%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.
Targets & IC50	CHO cells:3.44 μM (EC50), TGR5:0.82 μM (EC50), NCI-H716 cells:0.82 μM (EC50), HEK293 cells:0.36 μM (EC50), COS-1 cells:> 100 μM (EC50)
In vitro	Methods: Intestinal crypts isolated from wild-type and Tgr5 knockout mice were cultured into organoids. INT-777 (30μM) was added to the organoid culture medium and treated for 7 days, with organoid growth parameters (area, budding, etc.) observed. Results: INT-777 significantly promoted the growth of intestinal organoids derived from wild-type mice but had no such effect on organoids from Tgr5⁻/⁻ mice, confirming its TGR5-dependent action. [1] Methods: RAW264.7 mouse macrophages were stimulated with LPS (100 ng/mL) for 24 hours to induce M1 polarization. INT-777 (3 μM) was added 2 hours after LPS stimulation and co-incubated with cells for 24 hours. Results: Inhibited LPS-induced M1 polarization and promoted M2 polarization. [2]
In vivo	Methods: Adult male Sprague-Dawley rats were used. A rat subarachnoid hemorrhage (SAH) model was established via intravascular perforation. One hour after SAH, INT-777 (10, 30, 90 μg/kg) was administered intranasally, with Assess neurological function 24 hours later. Results: The 30 μg/kg dose proved most effective, significantly improving neurological function and reducing cerebral edema. [3]
Synonyms	S-EMCA

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.2190 mL	11.0951 mL	22.1902 mL	110.9508 mL
5 mM	0.4438 mL	2.2190 mL	4.4380 mL	22.1902 mL
10 mM	0.2219 mL	1.1095 mL	2.2190 mL	11.0951 mL
20 mM	0.1110 mL	0.5548 mL	1.1095 mL	5.5475 mL
50 mM	0.0444 mL	0.2219 mL	0.4438 mL	2.2190 mL

Ethanol

	1mg	5mg	10mg	50mg
100 mM	0.0222 mL	0.1110 mL	0.2219 mL	1.1095 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent 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 TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc