|2-呋喃甲酸|CsnPharm

CAS No.: 88-14-2

呋喃甲酸 Catalog No. CSN13069

Synonyms: Furan-2-carboxylic acid;2-Furancarboxylic acid;Pyromucic acid

Furan-2-carboxylic acid, a natural product isolated and purified from the herbs of Hexagonia speciosa with anti-bacterial effect, is also an orally active selective human cathepsin K inhibitor which may have the therapeutic potential for the treatment of diseases characterized by excessive bone loss including osteoporosis.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Cathepsin K is a cysteine proteinase regulating bone resorbing in osteoclasts. Furan-2-carboxylic acid is a selective inhibitor of human cathepsin K with an IC50 value of 11 nM, which is 39-fold more than against rat cathepsin K. Treatment of furan-2-carboxylic acid in rabbit unfractionated bone cells for 48 hours inhibited osteoclast-mediated release of C-telopeptide of type 1 collagen (CTx) in a concentration-dependent manner from 10 to 1000 nM. Furan-2-carboxylic acid suppressed bone resorption induced by rabbit osteoclasts with an IC50 value of 37 nM without affecting bone mineralization or the activity of cellular alkaline phosphatase in MC3T3-E1 cells. The inhibition of CTx release by furan-2-carboxylic acid was also observed in human PBMC-derived osteoclast-like cells with an IC50 value of 205 nM. Oral administration of furan-2-carboxylic acid significantly downregulated parathyroid hormone-induced bone resorption in thyroparathyroidectomized rats in a six-hour duration at dose-dependent manner from 10 to 100 mg/kg, which was indicated by the change of plasma concentration of calcium. Four-week oral treatment of 100 mg/kg furan-2-carboxylic acid twice daily completely inhibited ovariectomized-induced bone loss in 3-month-old rats as shown in bone densitometry, ash content, and urinary excretion of deoxypyridinoline.
作用机制Furan-2-carboxylic acid selectively prevents bone resorbing activities of osteoclasts and estrogen deficiency-induced bone loss through the inhibition of cathepsin K activity.
动物研究
剂量
Mice: 20 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Kim MK, Kim HD, et al. An orally active cathepsin K inhibitor, furan-2-carboxylic acid, 1-{1-[4-fluoro-2-(2-oxo-pyrrolidin-1-yl)-phenyl] -3-oxo-piperidin-4-ylcarbamoyl}-cyclohexyl)-amide (OST-4077), inhibits osteoclast activity in vitro and bone loss in ovariectomized rats. J Pharmacol Exp Ther. 2006 Aug;318(2):555-62.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 8.9222 mL
- 44.6110 mL
- 89.2220 mL
- 5 mM
- 1.7844 mL
- 8.9222 mL
- 17.8444 mL
- 10 mM
- 0.8922 mL
- 4.4611 mL
- 8.9222 mL

技术信息

CAS号

88-14-2

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H4O3

运输

蓝冰

分子量

112.08

别名

Furan-2-carboxylic acid;2-Furancarboxylic acid;Pyromucic acid;2-Carboxyfuran;α-furancarboxylic acid;α-furoic acid;alpha-Furancarboxylic acid;alpha-Furoic acid;Kyselina 2-furoova;糠酸;呋喃-2-羧酸

溶解度

DMSO	22.0 mg/mL (196.3 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

呋喃甲酸 Catalog No. CSN13069

靶点选择性

请登录您的专属账户

确认信息