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Abacavir Sulfate

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Chemical Structure| 188062-50-2 同义名 : ABC sulfate;Abacavir Hemisulfate;1592U89
CAS号 : 188062-50-2
货号 : A674299
分子式 : C28H38N12O6S
纯度 : 98%
分子量 : 670.743
MDL号 : MFCD04112763
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(74.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 30 mg/mL(44.73 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Abacavir Hemisulfate (ABC Sulfate) is a competitive and brain-penetrant reverse transcriptase inhibitor. Absolute bioavailability of oral abacavir hemisulfate was 83% and can be administered with or without meals[3]. Abacavir has been approved for treatment of HIV infection in combination with other anti-HIV agents. About 70% of patients receiving abacavir (300 mg b.i.d) had less than 400 copies/mL of HIV RNA at 16 weeks[4]. HIV-infected patients received therapy switch from tenofovir disoproxil fumatate and emtricitabine (TDF/FTC) to abacavir and lamivudine (ABC/3TC), after 3 months, the low-density lipoprotein (LDL), high-density lipoprotein (HDL), and total cholesterol (TC) levels increased by a median (interquartile range) of 17 (7, 32), 6 (2, 13), and 27 (10, 45) mg/dL, respectively[5]. Recently, Abacavir Hemisulfate showed effect on novel pneumonia caused by 2019-novel coronavirus.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00085943 HIV Infection ... 展开 >> Infection, Human Immunodeficiency Virus 收起 << Phase 3 Completed - -
NCT00002409 HIV Infections Phase 3 Completed - -
NCT02342769 - Active, not recruiting October 15, 2018 Germany ... 展开 >> GSK Investigational Site Freiburg, Baden-Wuerttemberg, Germany, 79106 GSK Investigational Site Mannheim, Baden-Wuerttemberg, Germany, 68161 GSK Investigational Site Stuttgart, Baden-Wuerttemberg, Germany, 70197 GSK Investigational Site Ulm, Baden-Wuerttemberg, Germany, 89081 GSK Investigational Site Muenchen, Bayern, Germany, 80331 GSK Investigational Site Muenchen, Bayern, Germany, 80336 GSK Investigational Site Muenchen, Bayern, Germany, 80801 GSK Investigational Site Frankfurt am Main, Hessen, Germany, 60590 GSK Investigational Site Frankfurt, Hessen, Germany, 60596 GSK Investigational Site Osnabrueck, Niedersachsen, Germany, 49090 GSK Investigational Site Aachen, Nordrhein-Westfalen, Germany, 52062 GSK Investigational Site Duesseldorf, Nordrhein-Westfalen, Germany, 40237 GSK Investigational Site Koeln, Nordrhein-Westfalen, Germany, 50674 GSK Investigational Site Mainz, Rheinland-Pfalz, Germany, 55116 GSK Investigational Site Magdeburg, Sachsen-Anhalt, Germany, 39120 GSK Investigational Site Berlin, Germany, 10243 GSK Investigational Site Berlin, Germany, 10405 GSK Investigational Site Berlin, Germany, 10707 GSK Investigational Site Berlin, Germany, 10777 GSK Investigational Site Berlin, Germany, 10961 GSK Investigational Site Berlin, Germany, 13347 GSK Investigational Site Berlin, Germany, 14057 GSK Investigational Site Chemnitz, Germany, 09111 GSK Investigational Site Dortmund, Germany, 44137 GSK Investigational Site Hamburg, Germany, 20099 GSK Investigational Site Hamburg, Germany, 20246 GSK Investigational Site Koeln, Germany, 50668 GSK Investigational Site Koeln, Germany, 50679 GSK Investigational Site Weimar, Germany, 99427 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.49mL

0.30mL

0.15mL

7.45mL

1.49mL

0.75mL

14.91mL

2.98mL

1.49mL
参考文献

[1]Arae H, Tateyama M, et al. Evaluation of the Lipid Concentrations after Switching from Antiretroviral Drug Tenofovir Disoproxil Fumarate/Emtricitabine to Abacavir Sulfate/Lamivudine in Virologically-suppressed Human Immunodeficiency Virus-infected Patients. Intern Med. 2016;55(23):3435-3440.

[2]Huff JR. New drugs-reports of new drugs recently approved by the FDA. Abacavir sulfate. Bioorg Med Chem. 1999 Dec;7(12):2667-9.

[3]Chittick GE, Gillotin C, McDowell JA, Lou Y, Edwards KD, Prince WT, Stein DS. Abacavir: absolute bioavailability, bioequivalence of three oral formulations, and effect of food. Pharmacotherapy. 1999 Aug;19(8):932-42. doi: 10.1592/phco.19.11.932.31568. PMID: 10453964.

[4]Huff JR. New drugs-reports of new drugs recently approved by the FDA. Abacavir sulfate. Bioorg Med Chem. 1999 Dec;7(12):2667-9. doi: 10.1016/s0968-0896(99)00242-4. PMID: 10658570.

[5]Arae H, Tateyama M, Nakamura H, Tasato D, Kami K, Miyagi K, Maeda S, Uehara H, Moromi M, Nakamura K, Fujita J. Evaluation of the Lipid Concentrations after Switching from Antiretroviral Drug Tenofovir Disoproxil Fumarate/Emtricitabine to Abacavir Sulfate/Lamivudine in Virologically-suppressed Human Immunodeficiency Virus-infected Patients. Intern Med. 2016;55(23):3435-3440. doi: 10.2169/internalmedicine.55.7518. Epub 2016 Dec 1. PMID: 27904105; PMCID: PMC5216139.