< 生产厂家价格 >

舒拉明钠

舒拉明钠用途

Suramin sodium salt是具有多种生物活性的多磺化萘基脲。 Suramin是DNA拓扑异构酶II抑制剂,IC50为5 μM。

点击显示

舒拉明钠名称

[ CAS 号 ]:
129-46-4

[ 中文名 ]:
苏拉明钠

[ 英文名 ]:
Suramin sodium

[中文别名 ]:

[英文别名 ]:

Suramin hexasodium salt
EINECS 204-949-3
Naphuride
Suramin sodium salt
Suramin sodium
Suramin (Sodium Salt)
Sodium suramin
suramine sodium
Suramine sodium salt
Suramin hexasodium

舒拉明钠生物活性

[ 描述 ]:

Suramin sodium salt是具有多种生物活性的多磺化萘基脲。 Suramin是DNA拓扑异构酶II抑制剂,IC50为5 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> P2Y受体

研究领域 >> 癌症

[ 靶点 ]

IC50: 5 μM (DNA topoisomerase II)[3]

[体外研究]

苏拉明抑制培养的HeLa细胞中的细胞增殖和DNA合成。通过40μM苏拉明完全消除SV40 DNA的复制。 DNA聚合酶α对较低浓度的苏拉明敏感(IC50 =8μM)比DNA聚合酶δ(IC50 =36μM)敏感,而DNA聚合酶β对药物相对不敏感(IC50为90μM)[1]。苏拉明是细菌RecA蛋白的DNA链交换和ATP酶活性的有效抑制剂。苏拉明抑制RecA催化的LexA阻遏蛋白水解切割。苏拉明这种抑制作用的机制涉及其拆解RecA-单链DNA细丝的能力[2]。苏拉明是核酶DNA拓扑异构酶II的有效抑制剂。苏拉明抑制纯化的酵母拓扑异构酶II,IC50约为5μM[3]。

[体内研究]

与对照大鼠相比,苏拉明治疗在第21天显示出较低的肺动脉压,右心室肥大和远端血管肌肉化值。苏拉明治疗抑制PA-SMC增殖并减弱炎症反应和胶原沉积[4]。

[激酶实验]

ATP酶测定在10μL反应混合物中进行，所述反应混合物含有20mM Tris-HCl（pH 7.5），1mM DTT，8mM MgCl2,5μMM13环状ssDNA，来自指定细菌物种的2.5μMRecA和增加浓度的苏拉明。通过加入2mM [α-32P] ATP引发反应，在37℃温育30分钟并通过加入25mM EDTA终止反应[2]。

[动物实验]

大鼠：为了评估苏拉明的潜在预防和疗效，在MCT注射后将大鼠随机分成4组。在预防策略中，治疗在第一天开始，并且一组每周两次静脉内接受10mg / kg苏拉明，持续3周，而第二组在相同时间点仅接受载体。为了评估苏拉明的潜在疗效，给予大鼠MCT并且不进行处理21天，然后将其随机分成两组，随后从第21天至第42天（包括苏拉明或载体）用苏拉明或载体治疗。从MCT注射的第21天到对应于治疗期的第42天评估苏拉明对存活的影响[4]。

[参考文献]

[1]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.

[2]. Nautiyal A, et al. Suramin is a potent and selective inhibitor of Mycobacterium tuberculosis RecA protein and the SOS response: RecA as a potential target for antibacterial drug discovery. J Antimicrob Chemother. 2014 Jul;69(7):1834-43.

[3]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.

[4]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.

[相关活性小分子]

N,N''-1,4-丁烷二基双[N'-(3-异异硫氰基苯基)硫脲 | 地夸磷索四钠 | 普拉格雷 | BPTU游离态 | AZD1283 | 苏拉明 | TAK-024

舒拉明钠物理化学性质

[ 分子式 ]:
C₅₁H₃₄N₆Na₆O₂₃S₆

[ 分子量 ]:
1429.171

[ 精确质量 ]:
1427.938599

[ PSA ]:
551.01000

[ LogP ]:
11.61040

[ 外观性状 ]:
白色

[ 储存条件 ]:
0-6°C

[ 水溶解性 ]:
可溶

舒拉明钠MSDS

详细MSDS(安全技术说明书)

舒拉明钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QM7000000

CHEMICAL NAME :: 1,3,5-Naphthylenetrisulfonic acid, 8,8'-(ureylenebis(m-phenylenecarbonylimino(4-methyl- m-phenylene)carbonylimino))di-, hexasodium salt

CAS REGISTRY NUMBER :: 129-46-4

LAST UPDATED :: 199512

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C51-H34-N6-O23-S6.6Na

MOLECULAR WEIGHT :: 1429.21

WISWESSER LINE NOTATION :: L66J BSWQ DSWQ GSWQ JMVR D1 CMVR CMVMR CVMR B1 EVM- JL66J BSWQ DSWQ GSWQ &-NA- 6

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 :: 750 mg/kg

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

REFERENCE :: BBRCA9 Biochemical and Biophysical Research Communications. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 136,64,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 620 mg/kg

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

REFERENCE :: 85KYAH "Merck Index; an Encyclopedia of Chemicals, Drugs, and Biologicals", 11th ed., Rahway, NJ 07065, Merck & Co., Inc. 1989 Volume(issue)/page/year: 11,1423,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 252 mg/kg/7W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes

REFERENCE :: IVIVE4 In Vivo. (POB 51359, Kiffisia, GR-145 10, Greece) V.1- 1987- Volume(issue)/page/year: 6,617,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1750 mg/kg/7D-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: BBRCA9 Biochemical and Biophysical Research Communications. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 136,64,1986

点击显示

舒拉明钠安全信息

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22:Harmful if swallowed. R36/38:Irritating to eyes and skin .

[ 安全声明 (欧洲) ]:
22-24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
QM7000000

舒拉明钠合成路线

详细合成路线

舒拉明钠上下游产品

舒拉明钠上游产品

舒拉明钠下游产品

舒拉明钠文献

Purinergic signaling via P2Y receptors up-mediates IL-6 production by liver macrophages/Kupffer cells.

J. Toxicol. Sci. 39(3) , 413-23, (2014)

Resident macrophages in the liver (Kupffer cells) produce various cytokines and chemokines, and have important roles in hepatitis and liver fibrosis. The cells are activated by various factors, for ex...

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Nat. Chem. Biol. 5 , 765-71, (2009)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened...

更多文献