规格 | 价格 | 库存 | 数量 |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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体外研究 (In Vitro) |
通过激动腺苷 A1 和 A2 受体,去纤维钠可限制炎症介质的释放,并减少细胞内粘附分子 1 的产生,从而具有抗炎作用[1]。去纤苷钠通过提高前列腺素I2和E2的合成并抑制纤溶酶原激活剂抑制剂1型活性,防止血小板聚集并促进纤溶[1]。此外,去纤苷钠促进组织因子途径抑制剂的合成,同时减少组织因子的产生,从而减少外源性凝血级联的激活和纤维蛋白沉积[1]。去纤苷钠可防止肿瘤坏死因子 α 介导的内皮细胞损伤以及氟达拉滨诱导的激活和死亡[1]。
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体内研究 (In Vivo) |
当在静脉内 (ic) 凝血酶 (100 μg/kg) 之前腹腔 (ic) 给药时,去纤苷钠(64 mg/kg 推注加 64 mg/kg/h,持续 1 小时)可显着降低凝血酶在兔中产生颅内血栓栓塞的能力[2]。在兔子静脉注射 (iv) 凝血酶之前,静脉注射 (iv) 去纤维蛋白多核苷酸(64 mg/kg 推注加 64 mg/kg/h,持续 1 小时)可大大减少放射性标记血小板在胸循环中的可逆积累。 2]。用去纤维蛋白多核苷酸(150-175 mg/kg,IV)预处理可显着减少小鼠静脉注射人凝血酶(1250 μg/kg)后死亡的大多数动物[2]。
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参考文献 |
[1]. May T Aziz, et al. Defibrotide: An Oligonucleotide for Sinusoidal Obstruction Syndrome. Ann Pharmacother. 2018 Feb;52(2):166-174.
[2]. W Paul, et al. The effect of defibrotide on thromboembolism in the pulmonary vasculature of mice and rabbits and in the cerebral vasculature of rabbits. Br J Pharmacol. 1993 Dec;110(4):1565-71. |
分子式 |
C20H21N4O6P
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分子量 |
average:16300Da
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CAS号 |
83712-60-1
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相关CAS号 |
83712-60-1(sodium);1118915-78-8 (free acid);1402907-09-8 (disodium);1118915-79-9 (monosodium);
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外观&性状 |
Powder form
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SMILES |
P(=O)(O)(O)OC1=CC(=C(C=C1C(C)C)C1=NNC(N1C1C=CC2=C(C=CN2C)C=1)=O)O
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别名 |
Defibrotide;1118915-78-8; UNII-E1942E7K32; STA-1474;Defibrotide sodium
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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 |
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 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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。 |
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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) 。