Art. -Nr.: HY-15677

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INT-777

(Synonyms: S-EMCA)

49 Cited Publications

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Based on 49 publication(s) in Google Scholar

INT-777 is a potent TGR5 agonist with an EC₅₀ of 0.82 μM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.87%
CAS. Nr.: 1199796-29-6
Formel: C₂₇H₄₆O₅
Molecular Weight:450.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

INT-777 Chemical Structure

CAS. Nr.: 1199796-29-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (49)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

INT-777 is a potent TGR5 agonist with an EC₅₀ of 0.82 μM^[1].

IC₅₀ & Target

EC50: 0.82 μM (TGR5)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	3.44 μM Compound: 8, S-EMCA, INT-777	Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay	[PMID: 20014870]
COS-1	EC₅₀	>100 μM Compound: 8, S-EMCA, INT-777	Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay	[PMID: 20014870]
HEK293	EC₅₀	0.36 μM Compound: 1, INT-777, S-EMCA	Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay	[PMID: 24007860]
HEK293	EC₅₀	1.23 μM Compound: 1, INT-777, S-EMCA	Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay	[PMID: 24007860]
HEK293	EC₅₀	293 nM Compound: INT-777	Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay	[PMID: 25082126]
NCI-H716	EC₅₀	0.82 μM Compound: 3, INT-777, S-EMCA	Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis	[PMID: 24900463]
NCI-H716	EC₅₀	13 μM Compound: 1, INT-777	Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production	[PMID: 23831134]

In Vitro

INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity^[1]. 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) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its chole-hepatic shunt pathway with a ductular absorption and a potent choleretic effect in HF-fed TGR5-Tg male mice^[1]. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high-fat feeding in TGR5-Tg mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1199796-29-6
Appearance Solid
Molecular Weight 450.65
Formel C₂₇H₄₆O₅
Color White to yellow
SMILES

O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@@H]4[C@H](C)C[C@H](C)C(O)=O)([H])C1
Synonyms

S-EMCA
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (49)

All WBIHC

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Journal Impact Factor

Immunity

Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome. [Abstract]

2016 Oct 18;45(4):944. PMID: 27760343

INT-777 purchased from MedChemExpress. Usage Cited in: Immunity. 2016 Oct 18;45(4):944. [Abstract]

INT-777, a semi-synthetic TGR5 agonist, markedly represses caspase-1 maturation and IL-1β or IL-18 but not the TNF-α secretion induced by Nigericin, similar to LCA. LPS-primed BMDMs are treated with different doses of INT-777 and then stimulated with Nigericin. Supernatants (SN) and cell extracts (Lysate) are analyzed by immunoblotting.
Cell Res

Virus-induced accumulation of intracellular bile acids activates the TGR5-β-arrestin-SRC axis to enable innate antiviral immunity. [Abstract]

2019 Mar;29(3):193-205. PMID: 30651583
Cell Host Microbe

Metabolic immaturity and breastmilk bile acid metabolites are central determinants of heightened newborn vulnerability to norovirus diarrhea. [Abstract]

2024 Aug 21:S1931-3128(24)00290-7. PMID: 39214086
Cell Host Microbe

Temporal Regulation of the Bacterial Metabolite Deoxycholate during Colonic Repair Is Critical for Crypt Regeneration. [Abstract]

2018 Sep 12;24(3):353-363.e5. PMID: 30122655
Nat Commun

Ursodeoxycholic acid reduces antitumor immunosuppression by inducing CHIP-mediated TGF-β degradation. [Abstract]

2022 Jun 14;13(1):3419. PMID: 35701426
Adv Sci (Weinh)

Conjugated Lithocholic Acid Activates Hepatic TGR5 to Promote Lipotoxicity and MASLD-MASH Transition by Disrupting Carnitine Biosynthesis. [Abstract]

2025 May 8:e2410602. PMID: 40344326
J Adv Res

A novel TGR5 agonist Sauchinone ameliorates IMQ induced murine psoriasis by regulating macrophage polarization. [Abstract]

2025 Apr 22:S2090-1232(25)00278-4. PMID: 40274226
Biomaterials

A novel Kupffer cell-targeting nanoparticle system to Mitigate alcohol-associated liver disease. [Abstract]

2026 Feb:325:123623. PMID: 40795708
J Biomed Sci

Activation of TGR5 protects blood brain barrier via the BRCA1/Sirt1 pathway after middle cerebral artery occlusion in rats. [Abstract]

2020 May 8;27(1):61. PMID: 32381096
J Hazard Mater

Bile acid metabolism is altered in learning and memory impairment induced by chronic lead exposure. [Abstract]

2024 Jun 5:471:134360. PMID: 38663295
Nat Cardiovasc Res

The gut microbiota-bile acid-TGR5 axis orchestrates platelet activation and atherothrombosis. [Abstract]

2025 Apr 11. PMID: 40217125
Pharmacol Res

GPBAR1 preserves neurite and synapse of dopaminergic neurons via RAD21-OPCML signaling: Role in preventing Parkinson's disease in mouse model and human patients. [Abstract]

2022 Oct:184:106459. PMID: 36152741
Int J Biol Sci

Lithocholic acid inhibits dendritic cell activation by reducing intracellular glutathione via TGR5 signaling. [Abstract]

2022 Jul 11;18(11):4545-4559. PMID: 35864954
J Am Soc Nephrol

Bile Acid G Protein-Coupled Membrane Receptor TGR5 Modulates Aquaporin 2-Mediated Water Homeostasis. [Abstract]

2018 Nov;29(11):2658-2670. PMID: 30305310

INT-777 purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2018 Nov;29(11):2658-2670. [Abstract]

Western blots show that INT-767, INT-777, and INT747 upregulate AQP2 protein expression.
Biol Psychiatry

Takeda G Protein-Coupled Receptor 5 Modulates Depression-like Behaviors via Hippocampal CA3 Pyramidal Neurons Afferent to Dorsolateral Septum. [Abstract]

2021 Jun 1;89(11):1084-1095. PMID: 33536132
Phytomedicine

Huodan Qinghua formula inhibits CD36 membrane localisation via the TGR5-DHHC4 pathway to ameliorate lipotoxic damage in diabetic cardiomyopathy. [Abstract]

2026 Jan 1:153:157761. PMID: 41678909
Phytomedicine

Red ginseng extracts ameliorate high-fat diet-induced obesity and insulin resistance by activating the intestinal TGR5-mediated bile acids signaling pathway. [Abstract]

2023 Oct:119:154982. PMID: 37531904
Free Radic Biol Med

Activation of TGR5 with INT-777 attenuates oxidative stress and neuronal apoptosis via cAMP/PKCε/ALDH2 pathway after subarachnoid hemorrhage in rats. [Abstract]

2019 Nov 1;143:441-453. PMID: 31493504
Br J Pharmacol

Cholinergic G protein-coupled bile acid receptor 1 (TGR5/GPBA) in the medial septal orchestrates adult hippocampal neurogenesis and cognition in Alzheimer's disease mice. [Abstract]

2025 Nov;182(21):5409-5429. PMID: 40926398
Brain Behav Immun

INT-777 attenuates NLRP3-ASC inflammasome-mediated neuroinflammation via TGR5/cAMP/PKA signaling pathway after subarachnoid hemorrhage in rats. [Abstract]

2021 Jan;91:587-600. PMID: 32961266
Cell Rep

Maternal diet shapes milk bile acids to regulate neonatal growth through TGR5. [Abstract]

2025 Dec 24;45(1):116744. PMID: 41447527
Cell Rep

Gut microbiota-mediated secondary bile acids regulate dendritic cells to attenuate autoimmune uveitis through TGR5 signaling. [Abstract]

2021 Sep 21;36(12):109726. PMID: 34551302
Mol Med

Sodium butyrate regulates macrophage polarization by TGR5/β-arrestin2 in vitro. [Abstract]

2025 Jan 29;31(1):31. PMID: 39881219
Phytother Res

Quercetin improves nonalcoholic fatty liver by ameliorating inflammation, oxidative stress, and lipid metabolism in db/db mice. [Abstract]

2019 Dec;33(12):3140-3152. PMID: 31452288
Front Immunol

Metabolite-Sensing G Protein Coupled Receptor TGR5 Protects Host From Viral Infection Through Amplifying Type I Interferon Responses. [Abstract]

2018 Oct 2:9:2289. PMID: 30333836

INT-777 purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Oct 2:9:2289. [Abstract]

Immunoblot analysis of p-IRF3 and p-AKT in lysates of peritoneal macrophages (PEMs) pretreated with MK2206 (3 μM) or INT-777 (500 μM) for 1 h, and then infected with vesicular stomatitis virus (VSV) for 8 h.
J Invest Dermatol

Bile Acids Improve Psoriasiform Dermatitis through Inhibition of IL-17A Expression and CCL20-CCR6-Mediated Trafficking of T Cells. [Abstract]

2022 May;142(5):1381-1390.e11. PMID: 34808237
Microb Biotechnol

Protective Effect of Pediococcus pentosaceus Li05 on Constipation via TGR5/TPH1/5-HT Activation. [Abstract]

2025 Nov;18(11):e70257. PMID: 41159760
Int J Mol Sci

Activation of the G Protein-Coupled Bile Acid Receptor TGR5 Modulates the HCP5/miR-139-5p/DDIT4 Axis to Antagonize Cervical Cancer Progression. [Abstract]

2024 Aug 16;25(16):8932. PMID: 39201624
PLoS Pathog

Bile acids promote the caveolae-associated entry of swine acute diarrhea syndrome coronavirus in porcine intestinal enteroids. [Abstract]

2022 Jun 13;18(6):e1010620. PMID: 35696443
Biomolecules

Significant Reduction of Chenodeoxycholic Acid and Glycochenodeoxycholic Acid in the Elderly with Severe COVID-19. [Abstract]

2025 Jun 28;15(7):943. PMID: 40723815
Eur J Pharmacol

TGR5 rescues renal ischemia-reperfusion injury by suppressing ferroptosis and cAMP/PKA/Nrf2 axis. [Abstract]

2026 Feb 15:1015:178597. PMID: 41587732
Int Immunopharmacol

Targeting TGR5 to mitigate liver fibrosis: Inhibition of hepatic stellate cell activation through modulation of mitochondrial fission. [Abstract]

2024 Aug 6:140:112831. PMID: 39111149
Int Immunopharmacol

TGR5 agonist INT-777 mitigates inflammatory response in human endometriotic stromal cells: A therapeutic implication for endometriosis. [Abstract]

2019 Jun:71:93-99. PMID: 30878820
Mol Neurobiol

The TGR5 Agonist INT-777 Promotes Peripheral Nerve Regeneration by Activating cAMP-dependent Protein Kinase A in Schwann Cells. [Abstract]

2023 Apr;60(4):1901-1913. PMID: 36593434
Cell Signal

Membrane receptor TGR5 upregulates IP3R-induced calcium overload: Key mechanism of bile acid-induced acute pancreatitis. [Abstract]

2026 Aug:144:112512. PMID: 41921768
Aquacult Rep

February 2022, 100997.
Toxicol Appl Pharmacol

A novel bile acid analog, A17, ameliorated non-alcoholic steatohepatitis in high-fat diet-fed hamsters. [Abstract]

2020 Oct 1;404:115169. PMID: 32738331
Am J Physiol Endocrinol Metab

Central lipid sensing pathways contribute to the control of puberty and its alterations in conditions of obesity. [Abstract]

2025 Apr 2. PMID: 40172224
Endocrine

TGR5 suppresses high glucose-induced upregulation of fibronectin and transforming growth factor-β1 in rat glomerular mesangial cells by inhibiting RhoA/ROCK signaling. [Abstract]

2016 Dec;54(3):657-670. PMID: 27470217

INT-777 purchased from MedChemExpress. Usage Cited in: Endocrine. 2016 Dec;54(3):657-670. [Abstract]

After the transfection, the GMCs are treated with 10 μM INT-777 or DMSO (control) upon HG stimulation for 24 h. Western blot is performed to measure the protein expressions of FN and TGF-β. Upon HG stimulation, INT-777 treatment alone can significantly reduce the FN and TGF-β1 protein expressions, and the effect is potentiated by TGR5 overexpression.
Tetrahedron

22 June 2022, 132901.
Biochem Biophys Res Commun

INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis. [Abstract]

2018 Sep 3;503(1):38-44. PMID: 29859191

INT-777 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44. [Abstract]

Representative immunohistochemistry images for RIP3 expression in the pancreas with the treatment of AP or AP plus INT-777.

INT-777 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44. [Abstract]

Western Blot analysis of RIP3, and p-MLKL protein expressions detected in pancreatic tissues with the treatment of AP or AP plus INT-777.
Ocul Immunol Inflamm

Decreased Expression of TGR5 in Vogt-Koyanagi-Harada (VKH) Disease. [Abstract]

2020;28(2):200-208. PMID: 30794473
Universidad de Córdoba

2025.
bioRxiv

2024 May 1.
SSRN

2024 Mar 13.
Preprints

2024 Jan 26.
Research Square Preprint

2021 Mar.
Oncotarget

The G-protein-coupled bile acid receptor Gpbar1 (TGR5) protects against renal inflammation and renal cancer cell proliferation and migration through antagonizing NF-κB and STAT3 signaling pathways. [Abstract]

2017 Apr 29;8(33):54378-54387. PMID: 28903349
Chinese Journal of Pathophysiology

2017, 33(2):239-243.

INT-777 purchased from MedChemExpress. Usage Cited in: Chinese Journal of Pathophysiology. 2017, 33(2):239-243.

The effects of TGR5 activation on the mRNA (A) and protein (B) expression of CaN in the mouse cardiomyocytes induced by high glucose (HG).

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (221.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 50 mg/mL (110.95 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2190 mL

11.0951 mL

22.1902 mL

5 mM

0.4438 mL

2.2190 mL

4.4380 mL

10 mM

0.2219 mL

1.1095 mL

2.2190 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 5

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 6

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

The experiments are carried out in STC-1 or NCI-H716 cells treated with vehicle (DMSO) or INT-777. INT-777 is assessed for its agonistic activity on TGR5. cAMP production is performed. Cytochrome C oxidase activity is evaluated by following the oxidation of fully reduced cytochrome C at 550 nm. ATP/ADP ratio and GLP-1 release is measured according to the manufacturer's instruction. Primary brown adipocytes are prepared and ileal explants are prepared.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Age-matched male mice are used for all experiments. Genetically engineered mouse models (GEMMs), i.e. TGR5-Tg and TGR5-/- mice are generated. Diet-induced obesity (DIO) in the GEMMs or C57BL/6J mice is induced by feeding 8-week-old mice with a HF-diet (60%Cal/fat, D12492) for at least 8 weeks, as mentioned in the text and figure legends. In the dietary intervention experiments, INT-777 is mixed with diet at the dose sufficient to reach an in vivo dose of 30mg/kg/d. Mouse phenotyping experiments are performed according to EMPRESS protocols and aimed to assess food and water intake, body composition, energy expenditure, glucose and lipid homeostasis, and plasma biochemistry.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pellicciari R, et al. Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem. 2009 Dec 24;52(24):7958-61. [Content Brief]

[2]. Thomas C, et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009 Sep;10(3):167-77. [Content Brief]

[3]. Duboc H, et al.Reduction of epithelial secretion in male rat distal colonic mucosa by bile acid receptor TGR5 agonist, INT-777: role of submucosal neurons. Neurogastroenterol Motil. 2016 Jun 3. doi: 10.1111/nmo. [Content Brief]

[4]. Baiqiang Li, et al. INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis. Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.2190 mL	11.0951 mL	22.1902 mL	55.4754 mL
	5 mM	0.4438 mL	2.2190 mL	4.4380 mL	11.0951 mL
	10 mM	0.2219 mL	1.1095 mL	2.2190 mL	5.5475 mL
	15 mM	0.1479 mL	0.7397 mL	1.4793 mL	3.6984 mL
	20 mM	0.1110 mL	0.5548 mL	1.1095 mL	2.7738 mL
	25 mM	0.0888 mL	0.4438 mL	0.8876 mL	2.2190 mL
	30 mM	0.0740 mL	0.3698 mL	0.7397 mL	1.8492 mL
	40 mM	0.0555 mL	0.2774 mL	0.5548 mL	1.3869 mL
	50 mM	0.0444 mL	0.2219 mL	0.4438 mL	1.1095 mL
	60 mM	0.0370 mL	0.1849 mL	0.3698 mL	0.9246 mL
	80 mM	0.0277 mL	0.1387 mL	0.2774 mL	0.6934 mL
	100 mM	0.0222 mL	0.1110 mL	0.2219 mL	0.5548 mL

Keywords

INT-777

49 Cited Publications

100 mg Angebot einholen

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INT-777

GPCR/G Protein Compound Library

Endocrinology Compound Library

Anti-Obesity Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Bile Acids Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) INT-777

Biologische Aktivität

Chemical Information

Publications (49)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INT-777

GPCR/G Protein Compound Library

Endocrinology Compound Library

Anti-Obesity Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Bile Acids Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) INT-777

Biologische Aktivität

Chemical Information

Publications (49)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INT-777 Related Classifications

HY-15677 Related Classifications