Cipemastat|190648-49-8|(Ro 32-3555)-陌孚医药/Medlife

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Cipemastat (Synonyms: Ro 32-3555)

目录号: PL07402 纯度: ≥99%

CAS No. :190648-49-8

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中文名称	Cipemastat
英文名称	Cipemastat
英文别名	1-Piperidinebutanamide,b-(cyclopentylmethyl)-N-hydroxy-g-oxo-a-[(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)methyl]-,(aR,bR)-;CIPEMASTAT;Ro 32-3555;(2R,3R)-3-(Cyclopentylmethyl)-N-hydroxy-4-oxo-4-(piperidin-1-yl)-2-[(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl]butanamide;1-Piperidinebutanamide, beta-(cyclopentylmethyl)-N-hydroxy-gamma-oxo-alpha-[(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)methyl]-, (alphaR,betaR)-;(αR,βR)-β-(Cyclopentylmethyl)-N-hydroxy-γ-oxo-α-[(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)methyl]-1-piperidinebutanamide;Trocade;02HQ4TYQ60;Cipemastat [USAN:INN];(2R,3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-piperidin-1-yl-2-[(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl]butanamide;Trocade (TN);Cipemastat (USAN/INN);GTPL6466;BDBM30344;(alphaR,betaR)-beta-(Cyclopentylmethyl)-gamma-oxo-alpha-((3,4,4-piperidinebutyrohydroxamic acid;RO32;cipémastat;cipemastatum;(2R,3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-(piperidin-1-yl)-2-((3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl)butanamide;ro 28-2653;Ro32-3555;TM4960900;Tyrphostin AG 1478 \|
Cas No.	190648-49-8
分子式	C₂₂H₃₆N₄O₅
分子量	436.55
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情	Cipemastat 是一种有效的、人胶原酶 (collagenase) 1，2，3的抑制剂，其 K_i 值分别为 3.0，4.4，3.4 nM。
生物活性	Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with K i s of 3.0, 4.4 and 3.4 nM, respectively.
性状	Solid
IC50 & Target[1][2]	collagenases 1 3.0 nM (Ki) collagenases 2 4.4 nM (Ki)
体外研究(In Vitro)	Cipemastat (Ro 32-3555) is a potent, competitive inhibitor of human matrix metalloproteinases. Cipemastat is selective for collagenase 1, 2 and 3 relative to related matrix metalloproteinases. Cipemastat is also a potent inhibitor of rat collagenase (IC50=44.7±3.4 nM (n=4)). In vitro cartilage degradation ± inhibited IL-1a induced cartilage degradation in vitro in a concentration-dependent manner with an IC50=60 nM. The inhibition is not mediated by a cytotoxic action on explant chondrocytes. Cipemastat, at all concentrations tested, fail to modify glucose utilization when compared to explants cultured in the presence of IL-La alone. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	The amount of hydroxyproline in non-implanted cartilage is 119.3±4.2 nM/mg and this decreases in cartilages implanted in vehicle-dosed animals to 53.6±7.1 nM/mg over a fourteen day period. Animals administered Cipemastat orally at doses of 2.5, 5, 10 and 25 mg/kg show statistically increased levels of implanted cartilage hydroxypro-line. Fourteen days after the second challenge injection of P. acnes, the area of cartilage most consistently affected by pannus is the lateral femoral condyle, which is the area analysed. In non-arthritic animals the mean cartilage area is 0.17±0.02 mm (n=5). In arthritic animals there is a significant decrease to a mean area of 0.086±0.01 mm (n=10). The group of animals dosed with Cipemastat (50 mg/kg, p.o.) show a significantly greater area of cartilage with a mean value of 0.126±0.012 mm (n=9). The pannus area in vehicle-dosed animals is
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；In solvent -80°C 6 months
参考文献	[1]. E J Lewis, et al. Ro 32-3555, an orally active collagenase inhibitor, prevents cartilage breakdown in vitro and in vivo. Br J Pharmacol. 1997 May; 121(3): 540–546.

溶解度数据	In Vitro: DMSO : 100 mg/mL (229.07 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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