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Clodronic acid disodium salt

Clodronic acid disodium salt (Lodronate) 是一种口服具有活力的破骨细胞骨吸收 (osteoclastic bone resorption) 的抑制剂，是一代双磷酸盐。它可用于高骨转换状态、Paget’s 病和溶骨性骨转移中。

CAS号

22560-50-5

分子式

CH4Cl2O6P0·2Na

主要靶点

Others

仅限科研使用

Cat No : CM00175

Print datasheet

Synonyms

氯屈膦酸二钠|Lodronate|Loron|Clodronate Disodium

验证数据展示

  • CAS No.: 22560-50-5

    Clodronic acid disodium salt
    CAS#: 22560-50-5

产品信息

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

CAS号 22560-50-5
分子式 CH4Cl2O6P0·2Na
主要靶点 Others
主要通路 其他
分子量 288.86
纯度 100.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 氯屈膦酸二钠|Lodronate|Loron|Clodronate Disodium

体外活性

Clodronate significantly decreases total viability of cultures of J774 cells with EC50 of 300 μM, while liposome-encapsulated Clodronate decreases total viability of cultures of J774 cells with EC50 of 1 μM. Clodronate and liposome-encapsulated Clodronate is metabolized to a nonhydrolyzable adenosine triphosphate (ATP) analog, adenosine 5'-(beta, gamma-dichloromethylene) triphosphate, which can be detected in J774 cell extracts by using fast protein liquid chromatography. [1] Clodronate induces apoptosis in isolated osteoclasts. Clodronate, when administered in liposomes, also induces apoptosis in rat peritoneal macrophages in vitro and in liver macrophages of mice in vivo but not in murine macrophage-like RAW-264 cells. [2] Clodronate delivered into macrophages by liposome will kill these cells as a result of intracellular accumulation and irreversible metabolic damage. [3] Clodronate encapsulated in liposomes (clodrolip) efficiently depletes the phagocytic cells in the murine F9 teratocarcinoma and human A673 rhabdomyosarcoma mouse tumour models resulting in significant inhibition of tumour growth ranging from 75 to >92%, depending on therapy and schedule. [4] Clodronate, a bisphosphonate that lacks a nitrogen, does not inhibit protein isoprenylation but can be metabolized intracellularly to a beta-gamma-methylene (AppCp-type) analog of ATP, which is cytotoxic to macrophages in vitro. Clodronate is metabolited to AppCCl(2)p, and AppCCl(2)p inhibits mitochondrial oxygen consumption by a mechanism that involves competitive inhibition of the ADP/ATP translocase. [5]

溶解度

DMSO:Insoluble,H2O:58.82 mg/mL (203.64 mM),Sonification is recommended.

参考文献

1.Frith JC, et al. J Bone Miner Res, 1997, 12(9), 1358-1367.
2.Selander KS, et al. Mol Pharmacol, 1996, 50(5), 1127-1138.
3.van Rooijen N, et al. J Immunol Methods, 1996, 193(1), 93-99.
4.Zeisberger SM, et al. Br J Cancer, 2006, 95(3), 272-281.
5.Lehenkari PP, et al. Mol Pharmacol, 2002, 61(5), 1255-1262.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2