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[CAS NO. 1199796-29-6] INT-777
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15677 |
| Brand: | MCE |
| CAS: | 1199796-29-6 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 450.65 |
| Molecular Formula | C27H46O5 |
| 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 |
27 Publications Citing Use of MCE
- [1]Cell Res. 2019 Mar;29(3):193-205.
- [2]Immunity. 2016 Oct 18;45(4):944.
- [3]Cell Host Microbe. 2018 Sep 12;24(3):353-363.e5.
- [4]Nat Commun. 2022 Jun 14;13(1):3419.
- [5]Biol Psychiatry. 2021 Jun 1;89(11):1084-1095.
- [6]J Am Soc Nephrol. 2018 Nov;29(11):2658-2670.
- [7]Cell Rep. 2021 Sep 21;36(12):109726.
- [8]J Invest Dermatol. 19 November 2021.
- [9]Brain Behav Immun. 2021 Jan;91:587-600.
- [10]PLoS Pathog. 2022 Jun 13;18(6):e1010620.
- [11]Free Radic Biol Med. 2019 Nov 1;143:441-453.
- [12]Pharmacol Res. 2022 Sep 21;106459.
- [13]J Biomed Sci. 2020 May 8;27(1):61.
- [14]Front Immunol. 2018 Oct 2;9:2289.
- [15]Int J Biol Sci. 2022 Jul 11;18(11):4545-4559.
- [16]Mol Neurobiol. 2023 Jan 3.
- [17]Phytother Res. 2019 Dec;33(12):3140-3152.
- [18]Int Immunopharmacol. 2019 Mar 14;71:93-99.
- [19]Toxicol Appl Pharmacol. 2020 Oct 1;404:115169.
- [20]Endocrine. 2016 Dec;54(3):657-670.
- [21]Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44.
- [22]Tetrahedron. 22 June 2022, 132901.
- [23]Aquacult Rep. February 2022, 100997.
- [24]Ocul Immunol Inflamm. 2019 Feb 22:1-9.
- [25]Research Square Preprint. 2021 Mar.
- [26]Oncotarget. 2017 Apr 29;8(33):54378-54387.
- [27]Chinese Journal of Pathophysiology. 2017, 33(2):239-243.
Summary
INT-777 is a potent TGR5 agonist with an EC 50 of 0.82 μM [1] .
IC50 & Target
EC50: 0.82 μM (TGR5) [1]
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] .
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 cholehepatic 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : ≥ 50 mg/mL ( 110.95 mM )
DMSO : ≥ 31 mg/mL ( 68.79 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
-
1.
Add each solvent one by one: 0.5% CMC-Na /saline water
Solubility: 5 mg/mL (11.10 mM); Suspension solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% EtOH >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution
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.
- [2] Thomas C, et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009 Sep;10(3):167-77.
- [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.
- [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.
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