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

Firuglipel 

Cat. No.: HY-109032 Purity: 99.21%
COA 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

Size Price Stock Quantity
5 mg USD 680 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5500 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

Molecular Weight

467.49

Formula

C25H26FN3O5

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (213.91 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
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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Product Name:
Firuglipel
Cat. No.:
HY-109032
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