规格 | 价格 | 库存 | 数量 |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
当二硫碳钠(二乙基二硫代氨基甲酸钠)与Cu2+溶液反应形成二乙基二硫代氨基甲酸铜络合物时,胶结率会增加[1]。二硫碳酸钠是一种具有有效抗氧化和螯合特性的化合物[2]。
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体内研究 (In Vivo) |
免疫反应受到抑制的老年和新生小鼠受益于二硫碳酸钠(二乙基二硫代氨基甲酸钠)。在不降低抗肿瘤活性的情况下,二乙基二硫代氨基甲酸钠可以保护动物免受顺铂肾毒性。二硫卡钠能够提高艾滋病模型的免疫力、延长生存期、减轻淋巴结肿大和高丙种球蛋白血症[2]。
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药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Rats receiving levels of 500 mg of dithiocarb in 1-2 mL water/kg body weight by gavage reached plasma levels of 2 mg/L dithiocarb in 3 hours. A half life for absorption of 26 minutes was determined when S-dithiocarb dissolved in 2M phosphate buffer was injected into the small intestinal lumen of adult male Wistar rats at a dose of 25 mg/kg. Within 15 minutes of dosing rats with 25 mg (222 moles S)/rat S-dithiocarb i.p., nonprotein bound radiolabel was detected in the plasma (1561 nmoles/mL plasma) and in the liver (3211 nmoles/g liver). A substantial amount (>45% within 15 minutes of dosing) of radioactivity also was found to be bound reversibly to soluble proteins of liver and plasma. A small amount (<0.1%) of unchanged dithiocarb was detected in the urine of rats receiving ip injections of 25 mg (35)S-dithiocarb/rat. One hr after dosing, 96.1% of the radiolabeled urinary metabolites was of S-glucuronide conjugate and 3.9% inorganic sulfate. Within 1 hr after dosing, 7% of the administered (35)S-dithiocarb was recovered as carbon disulfide in the expired air. For more Absorption, Distribution and Excretion (Complete) data for SODIUM DIETHYLDITHIOCARBAMATE (7 total), please visit the HSDB record page. Metabolism / Metabolites In rats, four metabolites, diethyldithiocarbamate, diethyldithiocarbamate-s-glucuronide, inorganic sulfate and carbon disulfide were identified; these are also metabolites of disulfiram. |
参考文献 |
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其他信息 |
Sodium diethyldithiocarbamate appears as odorless white or slightly brown or slightly pink crystals. (NTP, 1992)
Sodium diethyldithiocarbamate is an organic molecular entity. Ditiocarb Sodium is the sodium salt form of ditiocarb, an active metabolite of disulfiram, with potential antineoplastic and chemosensitizing activities. Upon administration, ditiocarb sodium may form a complex with copper (Cu), a metal that selectively accumulates in cancer cells. This complex may inhibit the nuclear factor-kB (NF-kB) pathway activated by tumor hypoxia, thereby inhibiting tumor cell growth. It may also reverse chemoresistance and enhance cytotoxicity of other chemotherapeutic agents. A chelating agent that has been used to mobilize toxic metals from the tissues of humans and experimental animals. It is the main metabolite of DISULFIRAM. Mechanism of Action Although the ability of disulfiram to inactivate CYP2E1 has been known for more than 20 years, the mechanism has not yet been elucidated. A metabolite of disulfiram, diethyldithocarbamate (DDC), is converted by CYP2E1 to a reactive intermediate that subsequently inactivates the protein, leading to mechanism-based inactivation. Mass spectral analysis of the inactivated human 2E1 protein demonstrates that the inactivation is due to the formation of an adduct of the reactive metabolite of DDC with the apoprotein. These data, along with mass spectral analysis of a reactive intermediate trapped with GSH, indicate the involvement of a reactive intermediate with a molecular mass of 116 Da. Our results suggest that this binding involves formation of a disulfide bond with one of the eight cysteines in CYP2E1. The inactivation of wild-type CYP2E1 as well as two of its polymorphic mutants, CYP2E1*2 and CYP2E1*4, was also investigated. For wild-type CYP2E1, the K(I) was 12.2 uM and the k(inact) was 0.02 min(-1). The K(I) values for the two polymorphic mutants were 227.6 and 12.4 uM for CYP2E1.2 and CYP2E1.4, and the k(inact) values were 0.0061 and 0.0187 min(-1), respectively. These data indicate that DDC is a much less efficient inactivator of CYP2E1.2 than it is of either the wild-type or the CYP2E1.4 variant. ... DDTC significantly inhibited the activity of superoxide dismutase and the activity of gamma-glutamyl transpeptidase, glutathione reductase, and alkaline phosphatase, whereas an increase in the activity of glutathione peroxidase was found. The membranes of pneumocytes type II were injured. |
分子式 |
C5H10NNAS2
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分子量 |
171.25
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精确质量 |
171.015
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CAS号 |
148-18-5
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相关CAS号 |
Ditiocarb;147-84-2;Ditiocarb-d10 sodium;1261395-23-6
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PubChem CID |
533728
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外观&性状 |
White to off-white solid powder
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密度 |
1.086g/cm3
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沸点 |
176.4ºC at 760mmHg
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熔点 |
95°C
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闪点 |
60.5ºC
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LogP |
1.81
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tPSA |
60.63
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氢键供体(HBD)数目 |
0
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氢键受体(HBA)数目 |
2
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可旋转键数目(RBC) |
2
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重原子数目 |
9
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分子复杂度/Complexity |
83
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定义原子立体中心数目 |
0
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SMILES |
[S-]C(N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=S.[Na+]
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InChi Key |
IOEJYZSZYUROLN-UHFFFAOYSA-M
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InChi Code |
InChI=1S/C5H11NS2.Na/c1-3-6(4-2)5(7)8;/h3-4H2,1-2H3,(H,7,8);/q;+1/p-1
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化学名 |
sodium;N,N-diethylcarbamodithioate
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别名 |
Ditiocarb sodium NSC-38583 NSC38583NSC 38583
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 请将本产品存放在密封且受保护的环境中,避免吸湿/受潮。 |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~100 mg/mL (~583.91 mM)
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (14.60 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (14.60 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (14.60 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 5.8394 mL | 29.1971 mL | 58.3942 mL | |
5 mM | 1.1679 mL | 5.8394 mL | 11.6788 mL | |
10 mM | 0.5839 mL | 2.9197 mL | 5.8394 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00000650 | COMPLETED | Drug: Ditiocarb sodium | HIV Infections | National Institute of Allergy and Infectious Diseases (NIAID) | 1996-09 | Not Applicable |
NCT00002069 | COMPLETED | Drug: Ditiocarb sodium | HIV Infections | Merieux Institute | Not Applicable | |
NCT02715609 | ACTIVE, NOT RECRUITING | Drug: Disulfiram Drug: Copper Gluconate Procedure: Surgery |
Glioblastoma Multiforme | Washington University School of Medicine | 2016-06-15 | Phase 1 Phase 2 |