129688-50-2

129688-50-2 structure

Name: Minalrestat
Chemical Name: 2-[(4-bromo-2-fluorophenyl)methyl]-6-fluorospiro[isoquinoline-4,3'-pyrrolidine]-1,2',3,5'-tetrone
CAS Number: 129688-50-2
Molecular Formula: C₁₉H₁₁BrF₂N₂O₄
Molecular Weight: 449.20200
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
Create Date: 2018-03-16 08:00:00
Modify Date: 2024-01-02 18:20:58
Minalrestat (ARI-509) is a potent and orally active aldose reductase inhibitor. Minalrestat can be used in the research of diabetes[1].

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

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.

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

HS Code	2933990090

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%

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