中文名 | 苏拉明钠 |
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英文名 | Suramin hexasodium salt |
中文别名 |
苏拉明
8,8'-碳酰双亚氨-3,1-亚苯基碳酰亚氨-(4-甲基-3,1-亚苯基)碳酰亚氨双-1,3,5-萘三磺酸六钠 舒拉明钠 |
英文别名 |
Hexasodium 8,8'-{carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]}di(1,3,5-naphthalenetrisulfonate)
Suramin hexasodium salt EINECS 204-949-3 Naphuride Hexasodium 8-[(4-methyl-3-{[3-({[3-({2-methyl-5-[(4,6,8-trisulfonato-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl]carbamoyl}amino)benzoyl]amino}benzoyl)amino]naphthalene-1,3,5-trisulfonate Suramin sodium salt Hexasodium sym-Bis(m-aminobenzoyl-m-amino-p-methylbenzoyl-1-naphthylamino-4,6,8-trisulfonate) Carbamide Suramin sodium hexasodium 8-[(4-methyl-3-{[3-({[3-({2-methyl-5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl}carbamoyl)phenyl]carbamoyl}amino)benzoyl]amino}benzoyl)amino]naphthalene-1,3,5-trisulfonate hexasodium,8-[[4-methyl-3-[[3-[[3-[[2-methyl-5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonate Suramin (Sodium Salt) Sodium suramin suramine sodium Suramine sodium salt Suramin hexasodium 1,3,5-Naphthalenetrisulfonic acid, 8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-, sodium salt (1:6) 309f MFCD00210217 |
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。 |
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相关类别 | |
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 |
分子式 | C51H34N6Na6O23S6 |
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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 |
计算化学 | 1.疏水参数计算参考值(XlogP):无 2.氢键供体数量:6 3.氢键受体数量:23 4.可旋转化学键数量:10 5.互变异构体数量:155 6.拓扑分子极性表面积551 7.重原子数量:92 8.表面电荷:0 9.复杂度:2940 10.同位素原子数量:0 11.确定原子立构中心数量:0 12.不确定原子立构中心数量:0 13.确定化学键立构中心数量:0 14.不确定化学键立构中心数量:0 15.共价键单元数量:7 |
Synonym: Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
Risk Phrases: None Listed. Section 3 - HAZARDS IDENTIFICATION EMERGENCY OVERVIEW
Not available. Potential Health Effects Eye: May cause eye irritation. Skin: May cause skin irritation. Ingestion: May cause irritation of the digestive tract. The toxicological properties of this substance have not been fully investigated. Inhalation: May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated. Chronic: Not available. Section 4 - FIRST AID MEASURES Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid. Skin: Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Ingestion: Get medical aid. Wash mouth out with water. Inhalation: Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid. Notes to Physician: Section 5 - FIRE FIGHTING MEASURES General Information: As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. Extinguishing Media: Use water spray, dry chemical, carbon dioxide, or chemical foam. Section 6 - ACCIDENTAL RELEASE MEASURES General Information: Use proper personal protective equipment as indicated in Section 8. Spills/Leaks: Vacuum or sweep up material and place into a suitable disposal container. Section 7 - HANDLING and STORAGE Handling: Avoid breathing dust, vapor, mist, or gas. Avoid contact with skin and eyes. Storage: Store in a cool, dry place. Store in a tightly closed container. Keep refrigerated. (Store below 4C/39F.) Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION Engineering Controls: Use adequate ventilation to keep airborne concentrations low. Exposure Limits CAS# 129-46-4: Personal Protective Equipment Eyes: Not available. Skin: Wear appropriate protective gloves to prevent skin exposure. Clothing: Wear appropriate protective clothing to prevent skin exposure. Respirators: Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Use a NIOSH/MSHA or European Standard EN 149 approved respirator if exposure limits are exceeded or if irritation or other symptoms are experienced. Section 9 - PHYSICAL AND CHEMICAL PROPERTIES Physical State: Powder Color: white Odor: Not available. pH: Not available. Vapor Pressure: Not available. Viscosity: Not available. Boiling Point: Not available. Freezing/Melting Point: Not available. Autoignition Temperature: Not available. Flash Point: Not available. Explosion Limits, lower: Not available. Explosion Limits, upper: Not available. Decomposition Temperature: Solubility in water: Soluble. Specific Gravity/Density: Molecular Formula: C51H34N6O23S6Na6 Molecular Weight: 1428.5632 Section 10 - STABILITY AND REACTIVITY Chemical Stability: Not available. Conditions to Avoid: Incompatible materials. Incompatibilities with Other Materials: Strong oxidizing agents. Hazardous Decomposition Products: Nitrogen oxides, carbon monoxide, oxides of sulfur, carbon dioxide, sodium oxide. Hazardous Polymerization: Will not occur. Section 11 - TOXICOLOGICAL INFORMATION RTECS#: CAS# 129-46-4: QM7000000 LD50/LC50: Not available. Carcinogenicity: Suramin.hexasodium salt - Not listed by ACGIH, IARC, or NTP. Other: See actual entry in RTECS for complete information. Section 12 - ECOLOGICAL INFORMATION Section 13 - DISPOSAL CONSIDERATIONS Dispose of in a manner consistent with federal, state, and local regulations. Section 14 - TRANSPORT INFORMATION IATA No information available. IMO No information available. RID/ADR No information available. Section 15 - REGULATORY INFORMATION European/International Regulations European Labeling in Accordance with EC Directives Hazard Symbols: Not available. Risk Phrases: Safety Phrases: S 24/25 Avoid contact with skin and eyes. WGK (Water Danger/Protection) CAS# 129-46-4: No information available. Canada None of the chemicals in this product are listed on the DSL/NDSL list. CAS# 129-46-4 is not listed on Canada's Ingredient Disclosure List. US FEDERAL TSCA CAS# 129-46-4 is not listed on the TSCA inventory. It is for research and development use only. SECTION 16 - ADDITIONAL INFORMATION N/A |
毒理学数据: 1、急性毒性:小鼠经腹腔LD5O:750mg/kg 小鼠经静脉LD5O:620mg/kg 2、其他多剂量毒性:大鼠经腹腔TDLO:252mg/m3/7W-I 小鼠经腹腔TDLO:1750mg/m3/7D-I
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
个人防护装备 | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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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 |
上游产品 1 | |
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下游产品 0 |