1. GPCR/G Protein
  2. GPR119

Firuglipel 

Cat. No.: HY-109032
Handling Instructions

Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.

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

Firuglipel Chemical Structure

Firuglipel Chemical Structure

CAS No. : 1371591-51-3

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.

IC50 & Target

GPR119[1]

In Vitro

Firuglipel (DS-8500a) increases intracellular cAMP in a concentration-dependent manner in human, rat, and mouse GPR119-expressing Chinese hamster ovary (CHO)-K1 cells, with EC50 values of 51.5, 98.4, and 108.1 nM, respectively. DS-8500a has no effect on intracellular cAMP in pcDNA3.1/CHO-K1 cells[1].

In Vivo

Firuglipel (DS-8500a) (1-30 mg/kg) upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1391 mL 10.6954 mL 21.3908 mL
5 mM 0.4278 mL 2.1391 mL 4.2782 mL
10 mM 0.2139 mL 1.0695 mL 2.1391 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]

Male SD rats (8 weeks) are fasted overnight and orally given vehicle (0.5% MC), DS-8500a (0.1, 1, 3 and 10 mg/kg), or glimepiride (10 mg/kg). Thirty minutes later, all animals received a 50% glucose solution intravenously (glucose load: 0.5 g/kg). Blood collection is performed from the tail vein 35 minutes before, 5 minutes before, and 5 minutes after the glucose load. The plasma insulin concentration is measured using ELISA kits.

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

References
Molecular Weight

467.49

Formula

C₂₅H₂₆FN₃O₅

CAS No.

1371591-51-3

SMILES

CC[[email protected]](C1=NC(C2=CC(F)=C(C(N[[email protected]](C)CO)=O)C=C2)=NO1)OC3=CC=C(C(C4CC4)=O)C=C3

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Firuglipel
Cat. No.:
HY-109032
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Firuglipel

Cat. No.: HY-109032