Cas No.: | 72702-95-5 |
Chemical Name: | 3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid |
SMILES: | C(CC(O)=O)1C2=C(C=CC=C2)C(=O)N(CC2=CC=C(Br)C=C2F)N=1 |
Formula: | C17H12BrFN2O3 |
M.Wt: | 391.2 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol[1][2][3]. |
Target: | Ki: 7.7 nM (ALR2) and 60 μM (ALR1)[1] |
In Vivo: | Statil (Ponalrestat; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition[3]. Animal Model: Adult female Sprague-Dawley rats[3] Dosage: 10, 50 mg/kg Administration: Orally; daily; 8 weeks Result: Reduced sorbitol accumulation. |
In Vitro: | Statil (Ponalrestat; 1, 10, 100 μM; 6 hours) reduces PGF2αproduction in response to IL-1 in both cultured endometrial cells and endometrial explants[2]. |
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. |