INT-777
Based on 48 publication(s) in Google Scholar
INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1199796-29-6
- Formula: C27H46O5
- Molecular Weight:450.65
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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GPCR/G Protein Compound Library
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HY-L001V
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HY-L208
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HY-L249
Publications Citing Use of MedChemExpress (MCE) INT-777
More- Immunity. 2016 Oct 18;45(4):944. [Abstract]
- Cell Res. 2019 Mar;29(3):193-205. [Abstract]
- Cell Host Microbe. 2024 Aug 21:S1931-3128(24)00290-7. [Abstract]
- Cell Host Microbe. 2018 Sep 12;24(3):353-363.e5. [Abstract]
- Nat Commun. 2022 Jun 14;13(1):3419. [Abstract]
- Adv Sci (Weinh). 2025 May 8:e2410602. [Abstract]
- J Adv Res. 2025 Apr 22:S2090-1232(25)00278-4. [Abstract]
- Biomaterials. 2026 Feb:325:123623. [Abstract]
- J Biomed Sci. 2020 May 8;27(1):61. [Abstract]
- J Hazard Mater. 2024 Jun 5:471:134360. [Abstract]
- Nat Cardiovasc Res. 2025 Apr 11. [Abstract]
- Pharmacol Res. 2022 Oct:184:106459. [Abstract]
- Int J Biol Sci. 2022 Jul 11;18(11):4545-4559. [Abstract]
- J Am Soc Nephrol. 2018 Nov;29(11):2658-2670. [Abstract]
- Biol Psychiatry. 2021 Jun 1;89(11):1084-1095. [Abstract]
- Phytomedicine. 2026 Jan 1:153:157761. [Abstract]
- Phytomedicine. 2023 Oct:119:154982. [Abstract]
- Free Radic Biol Med. 2019 Nov 1;143:441-453. [Abstract]
- Br J Pharmacol. 2025 Nov;182(21):5409-5429. [Abstract]
- Brain Behav Immun. 2021 Jan;91:587-600. [Abstract]
- Cell Rep. 2025 Dec 24;45(1):116744. [Abstract]
- Cell Rep. 2021 Sep 21;36(12):109726. [Abstract]
- Mol Med. 2025 Jan 29;31(1):31. [Abstract]
- Phytother Res. 2019 Dec;33(12):3140-3152. [Abstract]
- Front Immunol. 2018 Oct 2:9:2289. [Abstract]
- J Invest Dermatol. 2022 May;142(5):1381-1390.e11. [Abstract]
- Microb Biotechnol. 2025 Nov;18(11):e70257. [Abstract]
- Int J Mol Sci. 2024 Aug 16;25(16):8932. [Abstract]
- PLoS Pathog. 2022 Jun 13;18(6):e1010620. [Abstract]
- Biomolecules. 2025 Jun 28;15(7):943. [Abstract]
- Eur J Pharmacol. 2026 Feb 15:1015:178597. [Abstract]
- Int Immunopharmacol. 2024 Aug 6:140:112831. [Abstract]
- Int Immunopharmacol. 2019 Jun:71:93-99. [Abstract]
- Mol Neurobiol. 2023 Apr;60(4):1901-1913. [Abstract]
- Aquacult Rep. February 2022, 100997.
- Toxicol Appl Pharmacol. 2020 Oct 1;404:115169. [Abstract]
- Am J Physiol Endocrinol Metab. 2025 Apr 2. [Abstract]
- Endocrine. 2016 Dec;54(3):657-670. [Abstract]
- Tetrahedron. 22 June 2022, 132901.
- Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44. [Abstract]
- Ocul Immunol Inflamm. 2020;28(2):200-208. [Abstract]
- Universidad de Córdoba. 2025.
- bioRxiv. 2024 May 1.
- SSRN. 2024 Mar 13.
- Preprints. 2024 Jan 26.
- Research Square Preprint. 2021 Mar.
- Oncotarget. 2017 Apr 29;8(33):54378-54387. [Abstract]
- Chinese Journal of Pathophysiology. 2017, 33(2):239-243.
Customer Validation & Images
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IHC
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Biological Activity
EC50: 0.82 μM (TGR5)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
3.44 μM
Compound: 8, S-EMCA, INT-777
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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
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[PMID: 20014870] |
| COS-1 | EC50 |
>100 μM
Compound: 8, S-EMCA, INT-777
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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
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[PMID: 20014870] |
| HEK293 | EC50 |
0.36 μM
Compound: 1, INT-777, S-EMCA
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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
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[PMID: 24007860] |
| HEK293 | EC50 |
1.23 μM
Compound: 1, INT-777, S-EMCA
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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
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[PMID: 24007860] |
| HEK293 | EC50 |
293 nM
Compound: INT-777
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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
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[PMID: 25082126] |
| NCI-H716 | EC50 |
0.82 μM
Compound: 3, INT-777, S-EMCA
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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
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[PMID: 24900463] |
| NCI-H716 | EC50 |
13 μM
Compound: 1, INT-777
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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
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[PMID: 23831134] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1199796-29-6
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Appearance Solid
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Molecular Weight 450.65
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Formula C27H46O5
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Color White to yellow
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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
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Synonyms
S-EMCA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (48)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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
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
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.
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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 -
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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.
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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.
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Ocul Immunol Inflamm
2020;28(2):200-208. PMID: 30794473 -
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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 -
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).
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
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Data Sheet (281 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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