1. Metabolic Enzyme/Protease
    GPCR/G Protein
  2. FXR
    GPCR19

INT-767 

Cat. No.: HY-12434 Purity: >98.0%
Data Sheet SDS Handling Instructions

INT-767 is a potent agonist for both FXR (mean EC50, 30 nM by PerkinElmer AlphaScreen assay) and TGR5 (mean EC50, 630 nM by time resolved-fluorescence resonance energy transfer).

For research use only. We do not sell to patients.
INT-767 Chemical Structure

INT-767 Chemical Structure

CAS No. : 1000403-03-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $825 In-stock
5 mg $750 In-stock
10 mg $1200 In-stock
50 mg $3600 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

INT-767 is a potent agonist for both FXR (mean EC50, 30 nM) and TGR5 (mean EC50, 630 nM by time resolved-fluorescence resonance energy transfer). IC50 value: 30 nM (EC50, FXR), 630 nM (EC50, TGR5)[2] Target: FXR/TGR5 in vitro: INT-767 is the first compound described so far to potently and selectively activate both BA receptors. INT-767 significantly induces bile flow and biliary HCO3- output, as well as gene expression of carbonic anhy-drase 14, an important enzyme able to enhance HCO3- transport, in an Fxr-dependent manner[1]. INT-767 induces FXR-dependent lipid uptake by adipocytes, with the beneficial effect of shuttling lipids from central hepatic to peripheral fat storage, and promotes TGR5-dependent glucagon-like peptide-1 secretion by enteroendocrine cells, a validated target in the treatment of type 2 diabetes. INT-767 is a safe and effective modulator of FXR and TGR5-dependent pathways, suggesting potential clinical applications in the treatment of liver and metabolic diseases[2]. in vivo: INT-767 is a novel promising treatment in a mouse model of chronic cholangiopathy and characterized the underlying molecular and cellular mechanisms. INT-767 significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis in Mdr2-/-mice. INT-767 dramatically reduces bile acid synthesis via the induction of ileal Fgf15 and hepatic Shpgene expression, thus resulting in significantly reduced biliary bile acid output in Mdr2-/- mice[1]. Moreover, INT-767 treatment markedly decreases cholesterol and triglyceride levels in diabetic db/db mice and in mice rendered diabetic by streptozotocin administration[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0216 mL 10.1080 mL 20.2159 mL
5 mM 0.4043 mL 2.0216 mL 4.0432 mL
10 mM 0.2022 mL 1.0108 mL 2.0216 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

494.66

Formula

C₂₅H₄₃NaO₆S

CAS No.

1000403-03-1

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 205.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
INT-767
Cat. No.:
HY-12434
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