1. GPCR/G Protein
    Neuronal Signaling
  2. GPR119
  3. Firuglipel

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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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].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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
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