STATIL
STATIL Basic information
- Product Name:
- STATIL
- Synonyms:
-
- STATIL
- [3-(4-BROMO-2-FLUOROBENZYL)-4-OXO-3H-PHTHALAZIN-1-YL]ACETIC ACID
- Ponalrestat
- 3-(4-BROMO-2-FLUOROBENZYL)-4-OXO-3H-PHTHALAZIN-1-YL]ACETIC ACID (STATIL)
- 3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid
- ICI-128436
- ICI-plc
- MK-538
- CAS:
- 72702-95-5
- MF:
- C17H12BrFN2O3
- MW:
- 391.19
- Product Categories:
-
- Inhibitors
- Mol File:
- 72702-95-5.mol
STATIL Chemical Properties
- 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
Safety Information
- Risk Statements
- 36/37/38
- Safety Statements
- 26-36/37/39
STATIL Usage And Synthesis
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).
Uses
Statil is a knon aldose reductase inhibitor which blocks the conversion of glucose to sorbitol. In addition it suppresses cell cancer growth
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. |
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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STATIL(72702-95-5)Related Product Information
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- (2-FLUORO-BENZYL)-HYDRAZINE
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- CHEMBRDG-BB 5937785
- 4-BROMO-BENZYL-HYDRAZINE
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- 4-ETHYL-2H-PHTHALAZIN-1-ONE