72702-95-5

72702-95-5 structure

Name: Statil
Chemical Name: 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxophthalazin-1-yl]acetic acid
CAS Number: 72702-95-5
Molecular Formula: C₁₇H₁₂BrFN₂O₃
Molecular Weight: 391.191
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
Create Date: 2018-03-23 08:00:00
Modify Date: 2024-01-10 18:57:44
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].

Name	2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxophthalazin-1-yl]acetic acid
Synonyms	Ponalrestatum PONALRESTAT [3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazinyl]acetic acid 2-(2-Fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4-ylacetic Acid 1-Phthalazineacetic acid, 3-[(4-bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo- 3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic Acid 3-(4-bromo-2-fluorobenzyl)-4-oxo-3h-phthalazin-1-ylacetic acid statil [3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl]acetic acid Prodiax

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].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase Research Areas >> Metabolic Disease
Target	Ki: 7.7 nM (ALR2) and 60 μM (ALR1)[1]
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].
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.
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.

76283-09-5

25947-13-1

~52%

72702-95-5

Precursor 2
76283-09-5 25947-13-1
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%