[CAS NO. 72702-95-5] Ponalrestat
PRODUCTS SPECIFICATIONS [72702-95-5]
DESCRIPTION [72702-95-5]
Overview
| MDL | MFCD00204117 |
|---|---|
| Molecular Weight | 391.19 |
| Molecular Formula | C17H12BrFN2O3 |
| SMILES | OC(CC(C1=C2C=CC=C1)=NN(CC3=C(C=C(Br)C=C3)F)C2=O)=O |
Summary
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 ( K i =7.7 nM) over ALR1 ( K i =60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol [1] [2] [3] .
IC50 & Target
Ki: 7.7 nM (ALR2) and 60 μM (ALR1) [1]
In Vitro
Ponalrestat (ICI 128436; 1, 10, 100 μM; 6 hours) reduces PGF2αproduction in response to IL-1 in both cultured endometrial cells and endometrial explants
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ponalrestat (ICI 128436; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Adult female Sprague-Dawley rats [3] |
| Dosage: | 10, 50 mg/kg |
| Administration: | Orally; daily; 8 weeks |
| Result: | Reduced sorbitol accumulation. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 62.5 mg/mL ( 159.77 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5563 mL | 12.7815 mL | 25.5630 mL |
| 5 mM | 0.5113 mL | 2.5563 mL | 5.1126 mL |
| 10 mM | 0.2556 mL | 1.2782 mL | 2.5563 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.32 mM); Clear solution
References
- [1] Ward WH, et al. Ponalrestat: a potent and specific inhibitor of aldose reductase. Biochem Pharmacol. 1990 Jan 15;39(2):337-46.
- [2] Bresson E, et al. The human aldose reductase AKR1B1 qualifies as the primary prostaglandin F synthase in the endometrium. J Clin Endocrinol Metab. 2011 Jan;96(1):210-9.
- [3] Calcutt NA, et al. Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. Diabetologia. 2004 Apr;47(4):718-24.