Statil

Modify Date: 2024-01-10 18:57:44

Statil Structure
Statil structure
Common Name Statil
CAS Number 72702-95-5 Molecular Weight 391.191
Density 1.6±0.1 g/cm3 Boiling Point 576.3±60.0 °C at 760 mmHg
Molecular Formula C17H12BrFN2O3 Melting Point 184-186ºC (DEC.)
MSDS N/A Flash Point 302.4±32.9 °C

 Use of Statil


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].

 Names

Name 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxophthalazin-1-yl]acetic acid
Synonym More Synonyms

 Statil Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 576.3±60.0 °C at 760 mmHg
Melting Point 184-186ºC (DEC.)
Molecular Formula C17H12BrFN2O3
Molecular Weight 391.191
Flash Point 302.4±32.9 °C
Exact Mass 390.001526
PSA 72.19000
LogP 2.70
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.663
Storage condition -20°C

 Safety Information

Risk Phrases 36/37/38
Safety Phrases 26-36/37/39
HS Code 2933990090

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

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%

 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