MIV-247

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MIV-247 (MIV247) 是一种有效的、选择性的、口服活性的组织蛋白酶 S 抑制剂，Ki 为 2.1 nM（人组织蛋白酶 S）。

MIV-247 (MIV247)?is a potent, selective, orally active inhibitor of cathepsin S with Ki of 2.1 nM (human cathepsin S); displays high selectivity (>200-fold) overs other related cathepsins, inhibits mouse and cynomolgus monkey cathepsin S with Ki of 4.5 and 7.2 nM, respectively; attenuates mechanical allodynia alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects in mouse model of neuropathic pain.Asthma Discontinued.

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Oral administration of MIV-247 (100-200 μmol/kg) dose-dependently attenuates mechanical allodynia by up to approximately 50% reversal when given as a single dose or when given twice daily for 5 days. Cathepsin S inhibition with MIV-247 exerts significant antiallodynic efficacy alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects or inducing pharmacokinetic interactions.

MIV 247 | MIV247

Metabolic Enzyme/Protease

Cathepsin

Cathepsin

Inflammation/Immunology

Asthma

1352817-76-5

391.391

C17H24F3N3O4

>98% (HPLC)

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CC(C(=O)NC(CC1(CCCC1)F)C(=O)NC2(CCC2)C(=O)C(=O)N)(F)F

(S)-N-(1-(2-amino-2-oxoacetyl)cyclobutyl)-2-(2,2-difluoropropanamido)-3-(1-fluorocyclopentyl)propanamide

(-20℃)

With Ice Pack

≥ 2 years