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- 详细信息
- 技术资料
- 库存:
45
- 英文名:
Fosamprenavir Calcium Salt
- CAS号:
226700-81-8
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
5mg 10mg
商品属性:
产品描述:
分子式:C25H34CaN3O9PS
分子量:623.67
溶解度:<6.51 mg/mL in DMSO, <6.24 mg/mL in H2O, ≥ 40.1 mg/mL in EtOH with gentle warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
GW433908G is a selective inhibitor of antiretroviral protease with the concentration of 1395 mg nM once daily in clinical trial [1].Antiretroviral protease is a subfamily of protease inhibitors and plays a pivotal role in treating HIV/AIDS and HCV infection. It has been reported that drugs designed as protease inhibitors can prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles [2] [3].GW433908 is a potent antiretroviral protease inhibitor and has improved solubility than amprenavir capsules. Many clinical studies have been done to examine GE433908 safety and pharmacokinetic profiles. In healthy male volunteers, administered GW433908 as tablets or suspension, food had slight effect on its pharmacokinetics and with fewer tablets GW433908 were well tolerated and delivered plasma amprenavir concentrations equivalent to the recommended therapeutic amprenavir dose which may be of clinical benefit in the treatment of HIV infection [4]. As a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, GW433908 (1395 mg, QD) combined with efavirenz (200 mg, QD) decreased plasma APV exposure when tested with healthy volunteers [1].References:[1]. Wire, M.B., et al., Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers. Aids, 2004. 18(6): p. 897-907.[2]. Hamada, Y., et al., High incidence of renal stones among HIV-infected patients on ritonavir-boosted atazanavir than in those receiving other protease inhibitor-containing antiretroviral therapy. Clin Infect Dis, 2012. 55(9): p. 1262-9.[3]. Zheng, Y., et al., Antiretroviral therapy and efficacy after virologic failure on first-line boosted protease inhibitor regimens. Clin Infect Dis, 2014. 59(6): p. 888-96.[4]. Falcoz, C., et al., Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. J Clin Pharmacol, 2002. 42(8): p. 887-98.
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
使用方法:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
公司正在出售的产品:
| 货号 | CS-01Y64454 | 规格 | 5mg 10mg |
| CAS号 | 226700-81-8 | 分子量 | 623.67 |
| 含量 | >98.00% | 别名 | GW 433908G;Lexiva;GW433908G;GW-433908G |
| 分子式 | C25H34CaN3O9PS | 化学名 | calcium;[(2R,3S)-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-[[(3S)-oxolan-3-yl]oxycarbonylamino]-4-phenylbutan-2-yl] phosphate |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C25H34CaN3O9PS
分子量:623.67
溶解度:<6.51 mg/mL in DMSO, <6.24 mg/mL in H2O, ≥ 40.1 mg/mL in EtOH with gentle warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
GW433908G is a selective inhibitor of antiretroviral protease with the concentration of 1395 mg nM once daily in clinical trial [1].Antiretroviral protease is a subfamily of protease inhibitors and plays a pivotal role in treating HIV/AIDS and HCV infection. It has been reported that drugs designed as protease inhibitors can prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles [2] [3].GW433908 is a potent antiretroviral protease inhibitor and has improved solubility than amprenavir capsules. Many clinical studies have been done to examine GE433908 safety and pharmacokinetic profiles. In healthy male volunteers, administered GW433908 as tablets or suspension, food had slight effect on its pharmacokinetics and with fewer tablets GW433908 were well tolerated and delivered plasma amprenavir concentrations equivalent to the recommended therapeutic amprenavir dose which may be of clinical benefit in the treatment of HIV infection [4]. As a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, GW433908 (1395 mg, QD) combined with efavirenz (200 mg, QD) decreased plasma APV exposure when tested with healthy volunteers [1].References:[1]. Wire, M.B., et al., Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers. Aids, 2004. 18(6): p. 897-907.[2]. Hamada, Y., et al., High incidence of renal stones among HIV-infected patients on ritonavir-boosted atazanavir than in those receiving other protease inhibitor-containing antiretroviral therapy. Clin Infect Dis, 2012. 55(9): p. 1262-9.[3]. Zheng, Y., et al., Antiretroviral therapy and efficacy after virologic failure on first-line boosted protease inhibitor regimens. Clin Infect Dis, 2014. 59(6): p. 888-96.[4]. Falcoz, C., et al., Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. J Clin Pharmacol, 2002. 42(8): p. 887-98.
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
使用方法:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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Fosamprenavir Calcium Salt
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