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6-巯基嘌呤(一水合物)

6-巯基嘌呤(一水合物)用途

6-Mercaptopurine hydrate 是一种嘌呤类似物,是内源性嘌呤的拮抗剂且已被广泛用作抗白血病药物和免疫抑制药物。

6-巯基嘌呤(一水合物)名称

[ CAS 号 ]:
6112-76-1

[ 中文名 ]:
6-巯基嘌呤(一水合物)

[ 英文名 ]:
6-Mercaptopurine monohydrate

[中文别名 ]:

[英文别名 ]:

9H-purine-6-thiol, hydrate (1:1)
7H-purine-6-thiol, hydrate (1:1)
LEUKERIN MONOHYDRATE
6-Mercaptopurine monohydrate
6H-Purine-6-thione, 3,7-dihydro-, hydrate (1:1)
9H-Purine-6-thiol hydrate (1:1)
6MP H2O
MERCALEUKIN MONOHYDRATE
purin-6-thiol,monohydrate
1,7-Dihydro-6H-purine-6-thione hydrate (1:1)

6-巯基嘌呤(一水合物)生物活性

[ 描述 ]:

6-Mercaptopurine hydrate 是一种嘌呤类似物,是内源性嘌呤的拮抗剂且已被广泛用作抗白血病药物和免疫抑制药物。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

研究领域 >> 癌症

[ 靶点 ]

endogenous purines[1]

[体外研究]

6-巯基嘌呤水合物(6-MP)以剂量响应方式诱导NR-A3转录活性1.6至11倍(P <0.01)。发现6-巯基嘌呤水合物导致NR4A3蛋白水平的剂量依赖性增加。 6-巯基嘌呤水合物处理使基底细胞中的细胞表面GLUT4增加1.8至3.6倍(P <0.01),胰岛素刺激的细胞比对照增加2.9至4.4倍(P <0.01)。研究还发现,在基础和胰岛素刺激的条件下,6-巯基嘌呤水合物以剂量反应的方式显着增加磷酸化AS160 [2]。

[体内研究]

在6-巯基嘌呤水合物(6-MP)处理组的胎儿端脑中,S期细胞群在36和48小时时增加并在治疗后72小时恢复到对照水平。 G2/M期细胞群在24小时开始增加,在36小时达到峰值,在48小时时降低,最后在72小时返回到对照水平。另一方面,亚G1期细胞群(凋亡细胞)在36小时开始增加,在48小时达到峰值,然后在72小时开始减少[3]。

[激酶实验]

将L6肌管用DMSO对照或6-巯基嘌呤水合物（6-MP）处理24小时，最后3小时孵育包括在无血清DMEM中的处理，并在不存在或存在100nM胰岛素的情况下进一步孵育60小时。最低温度为37°C。然后，收集蛋白质裂解物（50μg）并进行SDS-PAGE。最后通过使用Image J软件[2]对扫描的薄膜进行光密度分析来定量蛋白质。

[细胞实验]

使用细胞活力测定法测量细胞活力。将L6骨骼肌细胞以10,000个细胞/孔的密度接种在96孔板中，并在7天内分化成肌管。在测定之前，用不同剂量的6-巯基嘌呤水合物（6-MP）处理细胞24小时。为了分析细胞活力，将板在室温下平衡30分钟;向每个孔中加入50μLCellTiter-Glo试剂，并将平板在轨道振荡器上混合12分钟。使用发光计[2]量化发光。

[动物实验]

在该研究中使用了大约13周龄的怀孕大鼠。将动物单独圈养在空调房间的线网笼中（温度23±3℃;湿度50±20％;通风，10次/小时;照明，12小时光照至12小时黑暗循环）和给予颗粒状饮食和随意饮水。在该实验中，15只怀孕的大鼠在E13上腹膜内注射50mg / kg的6-巯基嘌呤水合物（6-MP），并且在12,24,36,48下在乙醚麻醉下通过腹主动脉放血处死三只水坝。，72小时。通过剖腹产从每个大坝收集胎儿。作为对照，在E13下，向15只怀孕的大鼠腹膜内注射2.0％甲基纤维素的蒸馏水溶液，并在每个相同的时间点处死3只水坝[3]。

[参考文献]

[1]. Sahasranaman S, et al. Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67.

[2]. Liu Q, et al. 6-Mercaptopurine augments glucose transport activity in skeletal muscle cells in part via a mechanism dependent upon orphan nuclear receptor NR4A3. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1081-92.

[3]. Kanemitsu H, et al. 6-Mercaptopurine (6-MP) induces cell cycle arrest and apoptosis of neural progenitor cells in the developing fetal rat brain. Neurotoxicol Teratol. 2009 Mar-Apr;31(2):104-9.

[相关活性小分子]

6-巯基嘌呤(一水合物)物理化学性质

[ 沸点 ]:
490.6ºC at 760 mmHg

[ 熔点 ]:
>300 °C(lit.)

[ 分子式 ]:
C₅H₆N₄OS

[ 分子量 ]:
170.192

[ 闪点 ]:
250.5ºC

[ 精确质量 ]:
170.026230

[ PSA ]:
98.68000

[ LogP ]:
0.95120

[ 外观性状 ]:
淡黄色结晶粉末

[ 储存条件 ]:
Store at 0-5

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents, acids, strong bases. Light sensitive.

[ 水溶解性 ]:
INSOLUBLE

6-巯基嘌呤(一水合物)MSDS

详细MSDS(安全技术说明书)

6-巯基嘌呤(一水合物)毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UP0400000

CHEMICAL NAME :: Purine-6-thiol, monohydrate

CAS REGISTRY NUMBER :: 6112-76-1

LAST UPDATED :: 199410

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C5-H4-N4-S.H2-O

MOLECULAR WEIGHT :: 170.21

WISWESSER LINE NOTATION :: T56 BM DN FN HNJ ISH &QH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1250 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 224 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 27500 ug/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 500 mg/kg

SEX/DURATION :: male 40 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 250 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 4 mg/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg/40D (Intermittent)

REFERENCE :: DCTODJ Drug and Chemical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.1- 1977/78- Volume(issue)/page/year: 6,83,1983

6-巯基嘌呤(一水合物)安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S22-S36/37/39-S45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UP0400000

[ 海关编码 ]:
29335995

6-巯基嘌呤(一水合物)制备

1.可从7-氨基噻唑并[5,4-d]嘧啶制取，或从6-羟基嘌呤以硫化磷经置换制得。

2.以氰乙酸酯等为原料多步合成。

6-巯基嘌呤(一水合物)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%

6-巯基嘌呤(一水合物)文献

Primary sclerosing cholangitis, Crohn's disease and HLA-B27 in black South African women.

Acta Gastroenterol. Belg. 75(4) , 454-7, (2012)

Crohn's disease is rare in South African black people and primary sclerosing cholangitis (PSC) is also rare in black patients with IBD, from South Africa. The presence of HLA-B27 is generally associat...

In-vitro immunosuppression of canine T-lymphocyte-specific proliferation with dexamethasone, cyclosporine, and the active metabolites of azathioprine and leflunomide in a flow-cytometric assay.

Can. J. Vet. Res. 78(3) , 168-75, (2014)

A high rate of mortality, expense, and complications of immunosuppressive therapy in dogs underscores the need for optimization of drug dosing. The purpose of this study was to determine, using a flow...

[Peculiarities of extraction of 6-mercaptopurine and azathioprine from aqueous saline solutions].

Sud. Med. Ekspert. 55(6) , 38-41, (2012)

The results of extraction of 6-mercaptopurine and azathioprine from aqueous saline solutions with organic solvents of different chemical nature and their mixtures are presented. Synergism between the ...

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