CAS |
No.88416-50-6 |
中文名称 |
氯屈瞵酸二钠四水合物 |
英文名称 |
Clodronic acid disodium salt tetrahydrate |
别名 |
Clastoban |
分子式 |
CH12Cl2Na2O10P2 |
分子量 |
362.93 |
溶解性 |
Soluble in Water |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD02940846 |
SMILES |
C(P(=O)(O)[O-])(P(=O)(O)[O-])(Cl)Cl.O.O.O.O.[Na+].[Na+] |
InChIKey |
XWHPUCFOTRBMGS-UHFFFAOYSA-L |
InChI |
InChI=1S/CH4Cl2O6P2.2Na.4H2O/c2-1(3,10(4,5)6)11(7,8)9;;;;;;/h(H2,4,5,6)(H2,7,8,9);;;4*1H2/q;2*+1;;;;/p-2 |
PubChem CID |
23724874 |
靶点 |
Osteoclast |
通路 |
Immunology & Inflammation |
背景说明 |
是一种破骨细胞骨吸收 (osteoclastic bone resorption) 的抑制剂。 |
生物活性 |
Clodronic acid disodium salt tetrahydrate 是第一代双膦酸盐,具有抗骨质疏松、抗炎和镇痛作用。是一种选择性、强效、可逆、Cl-竞争性的囊泡核苷酸转运体(VNUT)抑制剂,IC50 为 15.6 nM。[1-2] |
In Vitro |
Clodronic acid disodium salt tetrahydrate inhibits VNUT at a half-maximal inhibitory concentration of 15.6 nM without affecting other vesicular neurotransmitter transporters,acting as an allosteric modulator through competition with Cl- A low concentration of clodronate impaired vesicular ATP release from neurons,microglia,and immune cells.[1] |
In Vivo |
Clodronic acid disodium salt tetrahydrate represent treatment for chronic neuropathic and inflammatory pain via inhibition of vesicular ATP release,in wild-type but not VNUT -/- mice,without affecting basal nociception.[1] |
数据来源文献 |
[1]. Kato Y,et al. Identification of a vesicular ATP release inhibitor for the treatment of neuropathic and inflammatory pain. Proc Natl Acad Sci U S A. 2017 Aug 1;114(31):E6297-E6305. [2]. Moriyama Y,et al. Clodronate: A Vesicular ATP Release Blocker. Trends Pharmacol Sci. 2018 Jan;39(1):13-23. |
规格 |
50mg 100mg 250mg |
单位 |
瓶 |