Minalrestat

Names

[ Name ]:
Minalrestat

[Synonym ]:
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

Biological Activity

[Description]:

Minalrestat (ARI-509) is a potent and orally active aldose reductase inhibitor. Minalrestat can be used in the research of diabetes[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase

Research Areas >> Metabolic Disease

[In Vitro]

Minalrestat (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 Vivo]

Minalrestat (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

[ Density]:
1.79g/cm3

[ Boiling Point ]:
707.4ºC at 760mmHg

[ Molecular Formula ]:
C₁₉H₁₁BrF₂N₂O₄

[ Molecular Weight ]:
449.20200

[ Flash Point ]:
381.6ºC

[ Exact Mass ]:
447.98700

[ PSA ]:
83.55000

[ LogP ]:
2.46090

[ Vapour Pressure ]:
7.38E-20mmHg at 25°C

[ Index of Refraction ]:
1.689

Safety Information

[ HS Code ]:
2933990090

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%