氯屈膦酸二钠

氯屈膦酸二钠用途

Clodronic acid (Clodronate) disodium salt,第一代双磷酸盐,一种具有口服活性的破骨细胞骨吸收 (osteoclastic bone resorption) 的抑制剂。Clodronic acid disodium salt 可用于高骨转换状态、Paget’s病和溶骨性骨转移中。

氯屈膦酸二钠名称

[ CAS 号 ]:
22560-50-5

[ 中文名 ]:
氯屈膦酸二钠

[ 英文名 ]:
Clodronate Disodium

[中文别名 ]:

[英文别名 ]:

Clastoban
Clodronic acid disodium salt
Bonefos
UNII-Y05R4GCQ1H
(Dichloromethylene)diphosphonic acid,disodium salt
EINECS 245-078-9
MFCD01632786
Clasteon
Lytos
Ossiten

氯屈膦酸二钠生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体外研究]

氯膦酸二钠盐(Clodronic acid,Clodronate)通过阻止ADP通过吸收内化进入线粒体而诱导破骨细胞快速凋亡。因此,ATP的产生受到抑制,通过将细胞色素C释放到细胞质中来诱导细胞凋亡[2]。

[体内研究]

氯膦酸(氯膦酸)二钠盐(6.25-25 mg/kg；p.o.；每日28天)在12.5和25 mg/kg的剂量下略微减少后爪肿胀[3]。动物模型：雄性Lewis大鼠,7周龄[3]剂量：6.25、12.5和25 mg/kg给药：P.o.；每日28天结果：后足肿胀明显小于佐剂性关节炎(AA)对照组,21天和28天分别为25 mg/kg(AA对照组的87%和88%)和28天为12.5 mg/kg。

[参考文献]

[1]. Mönkkönen J, et al. Clodronate (dichloromethylene bisphosphonate) inhibits LPS-stimulated IL-6 and TNF production by RAW 264 cells. Life Sci. 1994;54(14):PL229‐PL234.

[2]. Tanakol R, et al. Clodronic acid in the treatment of postmenopausal osteoporosis. Clin Drug Investig. 2007;27(6):419‐433.

[3]. Itoh F, et al. Effects of clodronate and alendronate on local and systemic changes in bone metabolism in rats with adjuvant arthritis. Inflammation. 2004;28(1):15‐21.

氯屈膦酸二钠物理化学性质

[ 密度 ]:
2.306g/cm3

[ 沸点 ]:
474.7ºC at 760mmHg

[ 熔点 ]:
>330ºC

[ 分子式 ]:
CH₂Cl₂Na₂O₆P₂

[ 分子量 ]:
288.856

[ 闪点 ]:
240.9ºC

[ 精确质量 ]:
287.849915

[ PSA ]:
140.34000

[ LogP ]:
1.30710

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
2.55E-10mmHg at 25°C

[ 储存条件 ]:
-20°C Freezer

氯屈膦酸二钠MSDS

详细MSDS(安全技术说明书)

氯屈膦酸二钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SZ7640700

CHEMICAL NAME :: Phosphonic acid, (dichloromethylene)bis-, disodium salt

CAS REGISTRY NUMBER :: 22560-50-5

LAST UPDATED :: 199512

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C-H2-Cl2-O6-P2.2Na

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3600 mg/kg/15D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - hematuria Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 17,27,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg/3D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - hematuria Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 17,27,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - pig

DOSE/DURATION :: 182 gm/kg/26W-I

TOXIC EFFECTS :: Musculoskeletal - changes in teeth and supporting structures Musculoskeletal - other changes Related to Chronic Data - death

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 59,129,1986

氯屈膦酸二钠安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
SZ7640700

[ 海关编码 ]:
2931900090

氯屈膦酸二钠海关

[ 海关编码 ]: 2931900090

[ 中文概述 ]:
2931900090. 其他有机-无机化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:AB(入境货物通关单,出境货物通关单). 最惠国关税:6.5%. 普通关税:30.0%

[ Summary ]:
2931900090. other organo-inorganic compounds. VAT:17.0%. Tax rebate rate:13.0%. Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward). MFN tariff:6.5%. General tariff:30.0%

氯屈膦酸二钠文献

Analysis of iminosugars and other low molecular weight carbohydrates in Aglaonema sp. extracts by hydrophilic interaction liquid chromatography coupled to mass spectrometry.

J. Chromatogr. A. 1423 , 104-10, (2015)

A method by hydrophilic interaction liquid chromatography coupled to tandem mass spectrometry (HILIC-MS(2)) has been successfully developed for the simultaneous analysis of bioactive iminosugars and o...

Phosphatase inhibitors with anti-angiogenic effect in vitro.

APMIS 118(1) , 49-59, (2010)

Levamisole has previously been identified as an inhibitor of angiogenesis in vitro and in vivo, but the mechanism behind the anti-angiogenic behavior has not yet been established. However, one known e...

CD11b⁺, Ly6G⁺ cells produce type I interferon and exhibit tissue protective properties following peripheral virus infection.

PLoS Pathog. 7(11) , e1002374, (2011)

The goal of the innate immune system is containment of a pathogen at the site of infection prior to the initiation of an effective adaptive immune response. However, effector mechanisms must be kept i...

更多文献