Clodronate Disodium

製品コードS4108 バッチS410801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	CH₄Cl₂O₆P₀.2Na
	分子量	288.86	CAS No.	22560-50-5
Solubility (25°C)*	体外	Water	72 mg/mL (249.25 mM)
		DMSO	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Clodronate Disodium, a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.
in vitro	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]

製品説明

Clodronate Disodium, a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

in vitro

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]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/9286751/
https://pubmed.ncbi.nlm.nih.gov/8913344/
https://pubmed.ncbi.nlm.nih.gov/8690935/

https://pubmed.ncbi.nlm.nih.gov/16832418/
https://pubmed.ncbi.nlm.nih.gov/11961144/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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