Dolutegravir-d5
(Synonyms: S/GSK1349572-d5) 目录号 : GC47261
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dolutegravir-d5 is intended for use as an internal standard for the quantification of dolutegravir by GC- or LC-MS. Dolutegravir is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.1 It inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). The cytotoxic concentration (CC50) values for dolutegravir in unstimulated and stimulated PBMCs are 189 and 52 µM, respectively, resulting in a therapeutic index of at least 9,400. It prevents replication of several HIV-1 strains (EC50s = 0.36-2.1 nM) that are resistant to nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors and impairs their ability to infect CIP4 cells.1,2 Formulations containing dolutegravir have been used to treat HIV-1 infection in humans.3
1.Kobyayshi, M., Yoshinaga, T., Seki, T., et al.In vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitorAntimicrob. Agents and Chemother.55(2)813-821(2011) 2.Hare, S.A., Smith, S.J., MÉtifiot , M., et al.Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572)Mol. Pharmacol.80(4)565-572(2011) 3.Venter, W.D.F., Clayden, P., and Serenata, C.The ADVANCE study: a groundbreaking trial to evaluate a candidate universal antiretroviral regimenCurr. Opin. HIV AIDS12(4)351-354(2017)
| Cas No. | N/A | SDF | |
| 别名 | S/GSK1349572-d5 | ||
| Canonical SMILES | FC1=C([2H])C(F)=C([2H])C([2H])=C1C([2H])([2H])NC(C2=CN(C[C@@](OCC[C@H]3C)([H])N3C4=O)C4=C(O)C2=O)=O | ||
| 分子式 | C20H14D5F2N3O5 | 分子量 | 424.4 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 2.5 mg/ml,Ethanol: Slightly Soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3563 mL | 11.7813 mL | 23.5627 mL |
| 5 mM | 0.4713 mL | 2.3563 mL | 4.7125 mL |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3563 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。