甲氨蝶呤二钠盐

甲氨蝶呤二钠盐用途

Methotrexate (Amethopterin) disodium 是一种抗代谢 (antimetabolite) 和抗叶酸(antifolate) 剂,可抑制二氢叶酸还原酶,从而防止叶酸转化为四氢叶酸并抑制 DNA 合成。Methotrexate disodium 也是一种免疫抑制剂和抗肿瘤剂,用于类风湿关节炎和研究多种癌症 (如急性淋巴细胞白血病)。

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甲氨蝶呤二钠盐名称

[ CAS 号 ]:
7413-34-5

[ 中文名 ]:
甲氨蝶呤二钠盐

[ 英文名 ]:
Methotrexate disodium

[中文别名 ]:

甲氨蝶呤二钠

[英文别名 ]:

METHOTREXATE DISODIUM
mtxdisodium
Methotrexate Disodium Salt Solution
amethopterinsodium
METHOTREXATUM
disodiummethotrexate
sodium methotrexate
l-(+)-isodiumsal

甲氨蝶呤二钠盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 叶酸

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素

研究领域 >> 炎症/免疫

[ 靶点 ]

Traditional Cytotoxic Agents

[体内研究]

甲氨蝶呤二钠降低小鼠胸腺和脾脏指数。剂量≥5mg/kg时,甲氨蝶呤二钠可显著降低白细胞、胸腺和脾脏淋巴细胞。治疗加对照组与模型组比较有显著性差异(p<0.01)。葡萄籽原花青素与西伯利亚人参皂甙合用可明显减轻甲氨蝶呤暴露对小鼠胸腺和脾脏指数的影响[2]。甲氨蝶呤(MTX)二钠(2mg/kg；一周一次,持续5周)对弗氏完全佐剂性关节炎有效。甲氨蝶呤二钠(1mg/kg；i.p.；一周一次,持续5周)和姜黄素(30mg/kg和100mg/kg,每周三次,持续5周；i.p.)的联合应用显示出显著的抗关节炎作用和防止血液毒性[4]。

[参考文献]

[1]. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73.

[2]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92.

[3]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92.

[4]. Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43(5):546-550.

甲氨蝶呤二钠盐物理化学性质

[ 沸点 ]:
823℃

[ 分子式 ]:
C₂₀H₂₀N₈Na₂O₅

[ 分子量 ]:
498.403

[ 精确质量 ]:
498.135193

[ PSA ]:
216.20000

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

甲氨蝶呤二钠盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MA1232000

CHEMICAL NAME :: Glutamic acid, N-(p-(((2,4-diamino-6-pteridinyl)methyl)methylamino)b enzoyl)-, disodium salt, L-(+)-

CAS REGISTRY NUMBER :: 7413-34-5

LAST UPDATED :: 199504

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C20-H20-N8-O5.2Na

MOLECULAR WEIGHT :: 498.46

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 284 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JNCIAM Journal of the National Cancer Institute. (Washington, DC) V.1-60, 1940-78. For publisher information, see JJIND8. Volume(issue)/page/year: 58,735,1977 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 120 mg/kg

SEX/DURATION :: male 60 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

REFERENCE :: JNCIAM Journal of the National Cancer Institute. (Washington, DC) V.1-60, 1940-78. For publisher information, see JJIND8. Volume(issue)/page/year: 58,735,1977 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5643 No. of Facilities: 4 (estimated) No. of Industries: 1 No. of Occupations: 15 No. of Employees: 1233 (estimated)

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甲氨蝶呤二钠盐安全信息

[ 海关编码 ]:
2933990090

甲氨蝶呤二钠盐合成路线

详细合成路线

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甲氨蝶呤二钠盐海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%