产品说明书
2-Furoic acid
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同义名 : | 糠酸 ;Furan-2-carboxylic acid;Pyromucic acid;Kyselina 2-furoova;alpha-Furoic acid;alpha-Furancarboxylic acid;α-furoic acid;α-furancarboxylic acid;2-Carboxyfuran;2-Furancarboxylic acid |
| CAS号 : | 88-14-2 | |
| 货号 : | A117549 | |
| 分子式 : | C5H4O3 | |
| 纯度 : | 95% | |
| 分子量 : | 112.08 | |
| MDL号 : | MFCD00003238 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(936.83 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 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. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
8.92mL 1.78mL 0.89mL |
44.61mL 8.92mL 4.46mL |
89.22mL 17.84mL 8.92mL |
| 参考文献 |
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