Cipemastat - CAS:190648-49-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Cipemastat
英文名称:	Cipemastat
别名:	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
CAS No:	190648-49-8	分子式:	C₂₂H₃₆N₄O₅	分子量:	436.55
CAS No:	190648-49-8
分子式:	C₂₂H₃₆N₄O₅
分子量:	436.55

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C11268 Cipemastat (psaitong)

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包装规格：

1mg in glass bottle

产品描述：

基本信息

产品编号：	C11268
产品名称：	Cipemastat
CAS:	190648-49-8	储存条件	粉末	-20℃	四年

分子式：	C22H36N4O5		溶于液体	-80℃	六个月
分子量	436.55			-20℃	一个月
化学名：	(2R,3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-piperidin-1-yl-2-[(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl]butanamide
Solubility (25°C)：
体外:	DMSO	100mg/mL(229.07mM;Need ultrasonic)
	Ethanol
	Water
体内(现配现用):	1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(5.73mM);Clear solution
	此⽅案可获得≥2.5mg/mL(5.73mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。
	2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(5.73mM);Clear solution
	此⽅案可获得≥2.5mg/mL(5.73mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。
	3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(5.73mM);Clear solution
	此⽅案可获得≥2.5mg/mL(5.73mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.2907mL	11.4534mL	22.9069mL
5mM	0.4581mL	2.2907mL	4.5814mL
10mM	0.2291mL	1.1453mL	2.2907mL

生物活性

产品描述	一种有效的、人胶原酶 (collagenase) 1，2，3的抑制剂。
靶点	collagenases 1 3.0nM (Ki)	collagenases 2 4.4nM (Ki)	collagenases 3 3.4nM (Ki)
	stromelysins 1 527nM (Ki)	gelatinase A 154nM (Ki)	gelatinase B 59.1nM (Ki)
体外研究	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±3.4nM (n=4)). In vitro cartilage degradation ± inhibited IL-1a induced cartilage degradation in vitro in a concentration-dependent manner with an IC50=60nM. 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
体内研究	The amount of hydroxyproline in non-implanted cartilage is 119.3±4.2nM/mg and this decreases in cartilages implanted in vehicle-dosed animals to 53.6±7.1nM/mg over a fourteen day period. Animals administered Cipemastat orally at doses of 2.5, 5, 10 and 25mg/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 mm2 (n=5). In arthritic animals there is a significant decrease to a mean area of 0.086±0.01 mm2 (n=10). The group of animals dosed with Cipemastat (50mg/kg, p.o.) show a significantly greater area of cartilage with a mean value of 0.126±0.012 mm2 (n=9). The pannus area in vehicle-dosed animals is 0.099±0.017 mm2 and in Cipemastat dosed animals 0.102±0.019 mm2 . Adjuvant arthritis injection of adjuvant induced two phases of swelling of the injected paw in vehicle-dosed rats. The primary swelling phase occurred between days 0 to 5 and induced an increase in paw volume of 1.9±0.1mL; the secondary phase occurrs between day 9 to 14 and there was an increase in paw swelling of 0.98±0.08mL. The group of animals dosed with dexamethasone (0.1mg/kg) shows a significant reduction in both primary (0.2±0.03mL) and secondary inflammation (0.07±0.08mL) paw swelling as well as total inhibition of the lesion score

推荐实验方法(仅供参考)

Animal Administration

Rats

Cipemastat (Ro 32-3555) is formulated in 5% succinylated gelatin and the volume administered to rats is 10mL/kg, p.o. Female, AHH/R strain rats are used. Rats are anaesthetized in an isoflurane-closed system, and an intra-articular injection of 20mL of the P. acnes/Freund's incomplete adjuvant emulsion made into the right hind knee. Twenty-eight days later the injection is repeated with the same volume and concentration of antigen to induce the monoarthritis. Animals are orally dosed once daily with either 5% succinylated gelatin as the control vehicle or Cipemastat (50mg/kg) starting on day 1 after challenge injection. Groups of eight female AHH/R rats are used in these experiments. The animals are dosed twice daily with either 50, 25 or 10mg/kg Cipemastat, dexamethasone (0.1mg/kg, s.c. once/day) or vehicle control (10mL/kg, p.o., b.i.d.). The arthritis is induced by injection into the right hind paws with 0.1mL of a 5mg/mL homogenized suspension of Mycobacterium tuberculosis in liquid paraffin. The volume of both the right and left hind paws is measured by water plethysmography by immersing the paw up to the hair line of the ankle. Paw volumes are determined every two or three days

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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