[CAS NO. 1371591-51-3] Firuglipel
PRODUCTS SPECIFICATIONS [1371591-51-3]
DESCRIPTION [1371591-51-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 467.49 |
| Molecular Formula | C25H26FN3O5 |
| SMILES | CC[C@H](C1=NC(C2=CC(F)=C(C(N[C@H](C)CO)=O)C=C2)=NO1)OC3=CC=C(C(C4CC4)=O)C=C3 |
Summary
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 EC 50 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.
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
DMSO : 100 mg/mL ( 213.91 mM ; Need ultrasonic)
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 |
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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