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  • 化合物 Cipemastat|T10817|TargetMol

化合物 Cipemastat|T10817|TargetMol

Cipemastat
190648-49-8
25500 100mg 起订
3750 5mg 起订
18600 50mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

VIP3年
联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 Cipemastat
英文名称:
Cipemastat
CAS号:
190648-49-8
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别:
抑制剂
货号:
T10817

Product Introduction

Bioactivity

名称Cipemastat
描述Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).
体外活性Cipemastat (Ro 32-3555) is also a potent inhibitor of rat collagenase (IC50: 44.7 nM). In vitro cartilage degradation ± inhibited IL-1a induced cartilage degradation in vitro in a concentration-dependent manner (IC50: 60 nM). The inhibition is not mediated by a cytotoxic action on explant chondrocytes. Cipemastat, at all concentrations tested, fails to modify glucose utilization when compared to explants cultured in the presence of IL-La alone.
体内活性The amount of hydroxyproline in non-implanted cartilage is 119.3 nM/mg and this decreases in cartilages implanted in vehicle-dosed animals to 53.6 nM/mg over a fourteen-day period. Animals administered Cipemastat orally at doses of 2.5, 5, 10, and 25 mg/kg showed statistically increased levels of implanted cartilage hydroxyproline. 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 analyzed. In arthritic animals, there is a significant decrease to a mean area of 0.086±0.01 mm2 (n=10). In non-arthritic animals, the mean cartilage area is 0.17±0.02 mm2 (n=5). 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 mm2 (n=9). The pannus area in vehicle-dosed animals is 0.099±0.017 mm2 and in Cipemastat dosed animals 0.102 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±0.1 mL; the second phase occurs between days 9 to 14 and there was an increase in paw swelling of 0.98±0.08 mL. The group of animals dosed with dexamethasone (0.1 mg/kg) shows a significant reduction in both primary (0.2±0.03 mL) and secondary inflammation (0.07±0.08 mL) paw swelling as well as total inhibition of the lesion score.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
关键字Cipemastat
Ro 32-3555|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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