KW-8232
目录号 : GC62667
KW-8232 是一种具有口服活性的抗骨质疏松剂，可以减少前列腺素 PGE2 的生物合成。
Cas No.:217813-15-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
KW-8232 is an anti-osteoporotic agent. KW-8232 reduces the biosynthesis of PGE2 in mouse osteoblastic cells[1].KW-8232 possesses anti-viral activity against SARS-CoV-2 (EC50 ~1.2 μM )[2].
KW-8232 (3, 10, 30 mg/kg, p.o.) potently increases the femoral bone mineral density (BMD) of immobilized legs of rats, and affects immobilization-induced abnormal bone turnovrer. KW-8232 markedly decreases urinary calcium excreation in the neurectomized rats only at 30 mg/kg, and highly reduces urinary pyridinoline and deoxypyridionline excretion which are markers of bone resorption in neurectomized rats. KW-8232 inhibits bone loss may be attributed to the lower prostaglandins (PGs)-stimulated bone resorption via regulation of PGE2 production[1].
[1]. Uchii M, et al. Effect of KW-8232, a novel anti-osteoporotic agent, on bone loss in sciatic neurectomized rats. Jpn J Pharmacol. 1998 Oct;78(2):241-3.
[2]. Shiwei Wang, et al. A Transferable Deep Learning Approach to Fast Screen Potent Antiviral Drugs against SARS-CoV-2. bioRxiv. 2020.
| Cas No. | 217813-15-5 | SDF | |
| 分子式 | C37H41ClN4O6S | 分子量 | 705.26 |
| 溶解度 | DMSO : 125 mg/mL (177.24 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4179 mL | 7.0896 mL | 14.1792 mL |
| 5 mM | 0.2836 mL | 1.4179 mL | 2.8358 mL |
| 10 mM | 0.1418 mL | 0.709 mL | 1.4179 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effect of KW-8232, a novel anti-osteoporotic agent, on bone loss in sciatic neurectomized rats
Jpn J Pharmacol 1998 Oct;78(2):241-3.PMID:9829630DOI:10.1254/jjp.78.241.
The purpose of this study was to evaluate the effects of 3-[bis(4-hydroxyphenyl)methyl]-2-[4-(2-chlorophenyl)-piperazin-1-+ ++ylcarbonyl]-1-(2-dimethylaminoethyl) indole methanesulfonate (KW-8232), a novel anti-osteoporotic agent, on bone loss in neurectomized rats. We also investigated the effect of KW-8232 on bone resorption in this animal model. Male Sprague-Dawley rats underwent unilateral hind-limb immobilization by sciatic neurectomy. KW-8232 (3, 10 and 30 mg/kg, p.o.) was effective in inhibiting femoral bone loss. KW-8232 decreased urinary pyridinoline and deoxypyridinoline excretion. These results indicate that KW-8232 effectively prevents the bone loss due to immobilization.
[Effect of KW-8232 on bone turnover in ovariectomized rats]
Nihon Yakurigaku Zasshi 1998 Nov;112(5):315-21.PMID:10098213DOI:10.1254/fpj.112.315.
The effects of 3-[bis(4-hydroxyphenyl)methyl]-2-[4-(2-chlorophenyl)- piperazin-1-ylcarbonyl]-1-(2-dimethylamino ethyl) indole methanesulfonate (KW-8232) on the bone turnover in ovariectomized (OVX) rats were studied by the oral administration for 6 weeks. KW-8232 inhibited the decreased bone mineral densities of the femur and tibia in OVX rats. OVX induced the increase of serum alkaline phosphatase and osteocalcin levels, markers of high bone turnover, and also increased urinary hydroxyproline, pyridinoline and deoxypyridinoline excretion, markers of bone resorption. KW-8232 significantly inhibited the increase of serum alkaline phosphatase level at doses of 10 and 30 mg/kg and the increase of osteocalcin level at a dose of 3 mg/kg. KW-8232 (1 mg/kg) markedly suppressed the OVX-induced increase of urinary hydroxyproline, pyridinoline and deoxypyridinoline excretion. KW-8232 didn't affect serum calcium level, but significantly decreased urinary calcium excretion at doses of 10 and 30 mg/kg. These results suggest that KW-8232 decreased bone loss in this model by suppressing bone resorption.