| Identification | Back Directory | [Name]
STATIL | [CAS]
72702-95-5 | [Synonyms]
STATIL
MK-538
ICI-plc
ICI-128436
Ponalrestat
Ponalrestat (MK-538
[3-(4-BROMO-2-FLUOROBENZYL)-4-OXO-3H-PHTHALAZIN-1-YL]ACETIC ACID
Ponalrestat Statil
3-(4-BROMO-2-FLUOROBENZYL)-4-OXO-3H-PHTHALAZIN-1-YL]ACETIC ACID (STATIL)
2-(3-(4-broMo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid
3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid | [Molecular Formula]
C17H12BrFN2O3 | [MDL Number]
MFCD00204117 | [MOL File]
72702-95-5.mol | [Molecular Weight]
391.19 |
| Chemical Properties | Back Directory | [Melting point ]
184-186℃ (DEC.) | [density ]
1.60 | [storage temp. ]
Store at RT | [solubility ]
DMF: 2 mg/mL; DMSO: 2 mg/mL; Ethanol: 2 mg/mL; PBS (pH 7.2): 0.2 mg/mL | [form ]
A crystalline solid | [color ]
White to off-white | [InChI]
InChI=1S/C17H12BrFN2O3/c18-11-6-5-10(14(19)7-11)9-21-17(24)13-4-2-1-3-12(13)15(20-21)8-16(22)23/h1-7H,8-9H2,(H,22,23) | [InChIKey]
LKBFFDOJUKLQNY-UHFFFAOYSA-N | [SMILES]
C12C=CC=CC=1C(=O)N(CC1=CC=C(Br)C=C1F)N=C2CC(=O)O |
| Hazard Information | Back Directory | [Description]
Statil is an aldose reductase inhibitor that blocks the conversion of glucose to sorbitol. It demonstrates selectivity for aldose reductase 2 over aldose reductase 1 with Ki values of 7.7 nM and 60 μM, respectively. Statil has been shown to prevent diabetes-induced alterations of the cardiovascular system in 14-day streptozotocin-diabetic rats. Aldose reductase inhibition by statil has also been used to impair the synthesis of prostaglandin F2α by human cultured preadipocytes. | [Uses]
Inhibitor (aldose reductase). | [Definition]
ChEBI: 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxo-1-phthalazinyl]acetic acid is a member of phthalazines. | [Biological Activity]
Potent aldose reductase inhibitor. | [in vivo]
Ponalrestat (ICI 128436; 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.
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| [References]
[1] WALTER H.J. WARD . Ponalrestat: A potent and specific inhibitor of aldose reductase[J]. Biochemical pharmacology, 1990, 39 2: Pages 337-346. DOI: 10.1016/0006-2952(90)90033-h
[2] DONNA J. OTTER Russell C W. The effects of aldose reductase inhibition with ponalrestat on changes in vascular function in streptozotocin diabetic rats[J]. British Journal of Pharmacology, 1994, 113 2: 576-580. DOI: 10.1111/j.1476-5381.1994.tb17028.x
[3] ANDRéANNE MICHAUD. Prostaglandin (PG) F2 alpha synthesis in human subcutaneous and omental adipose tissue: modulation by inflammatory cytokines and role of the human aldose reductase AKR1B1.[J]. PLoS ONE, 2014: e90861. DOI: 10.1371/journal.pone.0090861 |
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| Company Name: |
China Langchem Inc.
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0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0_EN.htm |
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