[CAS NO. 1199796-29-6] INT-777

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PRODUCTS SPECIFICATIONS [1199796-29-6]

Catalog

HY-15677

Brand

MCE

CAS

1199796-29-6

DESCRIPTION [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

For research use only. We do not sell to patients.

27 Publications Citing Use of MCE

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

In Vitro:

Ethanol : ≥ 50 mg/mL ( 110.95 mM )

DMSO : ≥ 31 mg/mL ( 68.79 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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.

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
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

* All of the co-solvents are available by MCE.