规格 | 价格 | 库存 | 数量 |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
HIV-1
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体外研究 (In Vitro) |
Nelfinavir (AG1341) Mesylate(1-10 μM;48 小时)可抑制多种骨髓瘤细胞的生长[4]。
Nelfinavir Mesylate 可抑制 26S 胰凝乳蛋白酶样蛋白酶体的活性,阻碍骨髓瘤细胞系增殖,并诱导细胞凋亡新生成的浆细胞[4]。 甲磺酸奈非那韦(1-10 μM;17 小时)细胞系在接触甲磺酸奈非那韦时会发生凋亡[4]。 甲磺酸奈非那韦(5 μM;0-24 小时)细胞凋亡减少AKT 磷酸化[4]。 甲磺酸奈非那韦导致 caspase-3 裂解,磷酸化 AKT、STAT-3 和 ERK1/2,并触发未折叠蛋白反应系统的促凋亡途径[4]。 Nelfinavir 的 IC50 为 35.93 μM,使其成为另一种 SARS-CoV 3CLpro 抑制剂[5]。 |
体内研究 (In Vivo) |
Nelfinavir Mesylate(75 mg/kg;腹腔注射;每周 5 天,持续 21 天)抑制 NOD/SCID 小鼠中多发性骨髓瘤细胞的生长。
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动物实验 |
NOD/SCID mice (bearing U266-luc cells)[4]
75 mg/kg I.p.; 5 days a week for 21 days |
参考文献 |
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分子式 |
C33H49N3O7S2
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分子量 |
663.8881
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精确质量 |
663.30
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元素分析 |
C, 59.70; H, 7.44; N, 6.33; O, 16.87; S, 9.66
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CAS号 |
159989-65-8
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相关CAS号 |
Nelfinavir;159989-64-7
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外观&性状 |
Solid powder
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SMILES |
CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC2=CC=CC=C2)[C@@H](CN3C[C@H]4CCCC[C@H]4C[C@H]3C(=O)NC(C)(C)C)O.CS(=O)(=O)O
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InChi Key |
NQHXCOAXSHGTIA-SKXNDZRYSA-N
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InChi Code |
InChI=1S/C32H45N3O4S.CH4O3S/c1-21-25(15-10-16-28(21)36)30(38)33-26(20-40-24-13-6-5-7-14-24)29(37)19-35-18-23-12-9-8-11-22(23)17-27(35)31(39)34-32(2,3)4;1-5(2,3)4/h5-7,10,13-16,22-23,26-27,29,36-37H,8-9,11-12,17-20H2,1-4H3,(H,33,38)(H,34,39);1H3,(H,2,3,4)/t22-,23+,26-,27-,29+;/m0./s1
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化学名 |
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide;methanesulfonic acid
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别名 |
Nelfinavir mesylate hydrate; AG-1343; AG1343; AG 1343; Nelfinavir; Viracept
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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 |
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) |
DMSO: ~100 mg/mL (~150.6 mM)
Ethanol: ~100 mg/mL (~150.6 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (3.77 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (3.77 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. 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 | 1.5063 mL | 7.5314 mL | 15.0627 mL | |
5 mM | 0.3013 mL | 1.5063 mL | 3.0125 mL | |
10 mM | 0.1506 mL | 0.7531 mL | 1.5063 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 |
NCT03829020 | Active Recruiting |
Drug: Nelfinavir Mesylate Drug: Bortezomib |
Recurrent Plasma Cell Myeloma Refractory Plasma Cell Myeloma |
Mayo Clinic | April 17, 2019 | Phase 1 |
NCT03256916 | Recruiting | Drug: Nelfinavir Drug: Cisplatin |
Carcinoma Cervix,Stage III | Tata Memorial Hospital | January 16, 2018 | Phase 3 |
NCT04169763 | Recruiting | Drug: Nelfinavir Drug: Cisplatin |
Stage II Vulvar Cancer AJCC v8 Stage III Vulvar Cancer AJCC v8 |
M.D. Anderson Cancer Center | August 7, 2020 | Phase 1 |
NCT05036226 | Recruiting | Combination Product: Hydroxychloroquine, Metformin, Sirolimus Combination Product: Hydroxychloroquine, Metformin, Sirolimus, Dasatanib |
Prostate Cancer Recurrent | Medical University of South Carolina |
March 3, 2022 | Phase 1 Phase 2 |
NCT00476606 | Active Recruiting |
Drug: Nevirapine, Efavirenz Drug: Zidovudine, Stavudine, Didanosine, Lamivudine |
HIV Infections | The HIV Netherlands Australia Thailand Research Collaboration |
March 2003 |
Nelfinavir inhibits proliferation of MM cell lines in vitro even in the presence of pro-survival cytokines. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir cooperates with anti-myeloma agents to inhibit the proliferation of multiple myeloma cells. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir induces the cleavage of pro-caspase 3 and apoptosis in MM cell lines. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir induces caspase-independent vacuolization and ER stress. Clin Cancer Res . 2007 Sep 1;13(17):5183-94. td> |
Nelfinavir inhibits NSCLC tumor growth in vivo, and induces markers of apoptosis, ER stress, and autophagy. Clin Cancer Res . 2007 Sep 1;13(17):5183-94. td> |
Effect of chronic exposure to nelfinavir (NEL) on insulin-induced nitric oxide (NO) production by human aortic endothelial cells. Ochsner J . 2013 Spring;13(1):76-90. td> |
Effect of chronic nelfinavir (NEL) exposure on the activation of second messengers of the insulin (INS) signaling cascade. Ochsner J . 2013 Spring;13(1):76-90. td> |