CAS 129688-50-2|Minalrestat

Introduction:Basic information about CAS 129688-50-2|Minalrestat, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameMinalrestat
CAS Number129688-50-2Molecular Weight449.20200
Density1.79g/cm3Boiling Point707.4ºC at 760mmHg
Molecular FormulaC19H11BrF2N2O4Melting Point/
MSDS/Flash Point381.6ºC

Names

Name2-[(4-bromo-2-fluorophenyl)methyl]-6-fluorospiro[isoquinoline-4,3'-pyrrolidine]-1,2',3,5'-tetrone
SynonymMore Synonyms

Minalrestat BiologicalActivity

DescriptionMinalrestat (ARI-509) is a potent and orally active aldose reductase inhibitor. Minalrestat can be used in the research of diabetes[1].
Related CatalogSignaling Pathways >>Metabolic Enzyme/Protease >>Aldose ReductaseResearch Areas >>Metabolic Disease
In VitroMinalrestat (100 μM) 减少原代培养的大鼠系细胞内山梨糖醇含量,而不影响的细胞内葡萄糖含量[3]。 Minalrestat (100 μM, 48 h) 在原代培养的大鼠系膜细胞中引起 PKC-α 和 -β2 的积累[3]。 Western Blot Analysis[3] Cell Line: Primary cultured rat mesangial cells Concentration: 100 μM Incubation Time: 48 h Result: Increased accumulation of PKC-α and -β2.
In VivoMinalrestat (口服灌胃,10 mg/kg/天,持续 30 天) 可恢复糖尿病大鼠中降低的微血管反应性[1]。 Minalrestat (口服灌胃,10 mg/kg) 可恢复糖尿病大鼠毛细血管后微静脉中减少的白细胞粘附和迁移白细胞数量[2]。 Animal Model: Alloxan (40 mg/kg i.v.)-induced diabetic rats[1] Dosage: 10 mg/kg/day Administration: Oral gavage, for 30 days. Result: Restored the decreased microvascular reactivity.
References

[1]. Akamine EH, et al. Minalrestat, an aldose reductase inhibitor, corrects the impaired microvascular reactivity in diabetes. J Pharmacol Exp Ther. 2003 Mar;304(3):1236-42.  

[2]. Cruz JW, et al. Minalrestat and leukocyte migration in diabetes mellitus. Diabetes Metab Res Rev. 2003 May-Jun;19(3):223-31.  

[3]. Kapor-Drezgic J, et al. Effect of high glucose on mesangial cell protein kinase C-delta and -epsilon is polyol pathway-dependent. J Am Soc Nephrol. 1999 Jun;10(6):1193-203.  

Chemical & Physical Properties

Density1.79g/cm3
Boiling Point707.4ºC at 760mmHg
Molecular FormulaC19H11BrF2N2O4
Molecular Weight449.20200
Flash Point381.6ºC
Exact Mass447.98700
PSA83.55000
LogP2.46090
Vapour Pressure7.38E-20mmHg at 25°C
Index of Refraction1.689
InChIKeyBMHZAHGTGIZZCT-UHFFFAOYSA-N
SMILESO=C1CC2(C(=O)N1)C(=O)N(Cc1ccc(Br)cc1F)C(=O)c1ccc(F)cc12

Safety Information

HS Code2933990090

Customs

HS Code2933990090
Summary2933990090. 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

Minalrestat (USAN/INN)
Minalrestat
WAY-ARI-509
Spiro(isoquinoline-4(1H),3'-pyrrolidine)-1,2',3,5'(2H)-tetrone,2-((4-Bromo-2-fluorophenyl)methyl)-6-fluoro
Bffipt
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