标签归档：卡韦

恩替卡韦

发表于由

恩替卡韦

货号：
IE1740

品牌：
Jinpan

恩替卡韦

暂无详情
产品简介
有效期 2年
EC EINECS 604-279-5
MDL MFCD00907887
别名 AIDS-098045
英文名称 Entecavir
CAS 142217-69-4
分子式 C12H15N5O3
分子量 277.28
储存条件 -20℃
纯度 ≥98%
外观（性状） Solid
单位 瓶
生物活性 Entecavir（SQ 34676; BMS 200475）是有选择且有效地HBV抑制剂。在HepG2细胞中的EC50值为3.75 nM。[1-3]
IC50 EC50: 3.75 nM (anti-HBV, HepG2 cell)[2]
In Vitro BMS-200475对HBV的EC50为3.75 nM。将其掺入HBV的蛋白质引物中，随后抑制逆转录酶的引发步骤。 BMS-200475的抗病毒活性明显低于其他RNA和DNA病毒[1]。与其他脱氧鸟苷类似物（喷昔洛韦，更昔洛韦，lobucavir和阿昔洛韦）或拉米夫定相比，恩替卡韦更容易被磷酸化为其活性代谢物。恩替卡韦的细胞内半衰期为15小时[2]。
In Vivo BMS-200475每日口服治疗，剂量范围为0.02至0.5毫克/千克体重，持续1至3个月，可有效降低慢性感染土拨鼠中土拨鼠肝炎病毒（WHV）病毒血症的水平[3]。
SMILES O=C1NC(N)=NC2=C1N=CN2[C@@H]3C([C@H](CO)[C@@H](O)C3)=C
靶点 HBV
细胞实验 BMS 200475在磷酸盐缓冲盐水（PBS）中制备，并用含有2％胎牛血清的适当培养基稀释。将HepG2 2.2.15细胞以每孔5×10 5个细胞的密度接种在12孔Biocoat胶原包被的平板上，并保持在融合状态2至3天，然后用1mL掺有BMS 200475的培养基覆盖。 HBV的定量在第10天进行[1]。
数据来源文献 [1]. Innaimo SF, et al. Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-9.
[2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin. 2005 Nov;21(11):1845-57.
[3]. Genovesi EV, et al. Efficacy of the carbocyclic 2′-deoxyguanosine nucleoside BMS-200475 in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother. 1998 Dec;42(12):3209-18
规格 10mg 25mg

是有选择性、有效的HBV抑制剂。

阿巴卡韦

发表于由

阿巴卡韦

货号：
IA4710

品牌：
Jinpan

阿巴卡韦

暂无详情
产品简介
有效期 2年
描述 是有效的核苷类似物逆转录酶抑制剂 (NRTI)。
EC EINECS 620-487-9
MDL MFCD00903850
别名 阿巴卡维
英文名称 Abacavir
CAS 136470-78-5
分子式 C14H18N6O
分子量 286.33
储存条件 2-8℃
纯度 ≥98%
外观（性状） Solid
单位 瓶
生物活性 Abacavir (1592U89, ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.[1-3]
In Vitro Abacavir (ABC) exhibits potent in vitro antiviral activity against wild-type HIV-1 (IC50 4.0 μM, MT-4 cells)[1]. Abacavir induces chromosomal DSBs and thereby kills ATL cells but not non-HTLV-1-infected cells. Once abacavir is incorporated into the cells, it is phosphorylated in a unique stepwise anabolism to be converted to the triphosphated guanine analog carbovir (CBV) and then incorporated into host chromosomal DNA by replicative DNA polymerases, leading to premature termination of DNA replication, collapse of the replication fork, and DSB formation. Abacavir induces S/G2-phase arrest and apoptosis in ED-40515(?) cells, but not in Jurkat cells[2].
In Vivo Abacavir efficiently inhibits the growth of ATL cell xenografts in NOD/SCID mice[2]. In adults, Abacavir is rapidly absorbed after oral administration, with peak concentrations occurring 0.63-1 hour after dosing. The absolute bioavailability of abacavir is approximately 83%. Abacavir pharmacokinetics are linear and doseproportional over the range of 300-1200 mg/day. The apparent volume of distribution of abacavir after intravenous administration is approximately 0.86 ± 0.15 L/kg, suggesting that abacavir is distributed to extravascular spaces. Binding to plasma proteins is about 50% and is independent of the plasma abacavir concentration. Abacavir is extensively metabolized by the liver; less than 2% is excreted as unchanged drug in the urine. Abacavir is primarily metabolized via two pathways, uridine diphosphate glucuronyltransferase and alcohol dehydrogenase, resulting in the inactive glucuronide metabolite and the inactive carboxylate metabolite. The terminal elimination half-life of abacavir is approximately 1.5 hours. The antiviral effect of abacavir is due to its intracellular anabolite, carbovirtriphosphate (CBV-TP). Abacavir is not significantly metabolized by cytochrome P450 (CYP) enzymes, nor does it inhibit these enzymes[3].
SMILES OC[C@@H]1C=C[C@H](N2C=NC3=C(NC4CC4)N=C(N)N=C23)C1
靶点 Reverse Transcriptase
动物实验 Cell lines: Jurkat cells; Concentrations: 300 μM; Incubation Time: 48 h; Method: Jurkat cells transfected with control siRNA or siTDP1 are treated with or without 300 μM ABC for 48 hours. MTS assay is conducted.[2]
细胞实验 Animal Models: NOD/SCID mice; Dosages: 75 mg/kg; Administration: oral[2]
数据来源文献 [1] Melroy J, et al. Curr Pharm Des. 2005, 11(29):3847-52.
[2] Tada K, et al. Sci Adv. 2015, 1(3):e1400203.
[3] Yuen GJ, et al. Clin Pharmacokinet. 2008, 47(6):351-71.
规格 10mg 25mg 50mg

恩替卡韦 标准品

发表于由

恩替卡韦 标准品

货号：
YZ-101248

品牌：
中检所

恩替卡韦 标准品

暂无详情
产品简介
CAS 209216-23-9
分子式 C12H15N5O3·H2O
分子量 295.29
储存条件 避光,10-30℃保存。
规格 50mg
别名：9-(4-羟基-3-羟甲基-2-亚甲基环戊-1-基)鸟嘌呤;恩替卡韦;2-氨基-9-((1S,3R,4S)-4-羟基-3-(羟甲基)-2-甲烯基环戊基)-3H-嘌呤-6(9H)-酮;恩替卡韦-D2;Entecavir;Entecavir Baraclude;2-Amino-1,9-Dihydro-9-[(1S,3R,4S)-4-Hydroxy-3-(Hydroxymethyl)-2-Methyle

熔点：249-252°C

硫酸阿巴卡韦

发表于由

硫酸阿巴卡韦

货号：
IA4700

品牌：
Jinpan

硫酸阿巴卡韦

暂无详情
产品简介
有效期 2年
描述 是核苷类似物逆转录酶抑制剂（NRTI），可用于HIV和AIDS的相关研究。
EC EINECS 620-488-4
MDL MFCD04112763
别名 阿巴卡韦硫酸盐；赛进
英文名称 Abacavir Sulfate
CAS 188062-50-2
分子式 C28H36N12O2·H2SO4
分子量 670.74
储存条件 -20℃
纯度 ≥98%
外观（性状） Solid
单位 瓶
生物活性 Abacavir is a nucleoside reverse transcriptase inhibitor marketed the treatment of infection with the human immunodeficiency virus type 1 (HIV). [1] Abacavir is a carbocyclic 2′-deoxyguanosine nucleoside analogue. It is metabolised intracellularly to a 2′-deoxyguanosine nucleoside analogue which competitively inhibits HIV reverse transcriptase and terminates proviral DNA chain extension. [2]
SMILES NC1=NC(NC2CC2)=C3N=CN([C@H]4C=C[C@@H](CO)C4)C3=N1.O=S(O)(O)=O.NC5=NC(NC6CC6)=C7N=CN([C@H]8C=C[C@@H](CO)C8)C7=N5
靶点 Reverse Transcriptase
数据来源文献 [1]. Charneira C, et al. Reactive aldehyde metabolites from the anti-HIV drug abacavir: amino acid adducts as possible factors in abacavir toxicity. Chem Res Toxicol. 2011 Dec 19;24(12):2129-41.
[2]. Hervey PS, et al. Abacavir: a review of its clinical potential in patients with HIV infection. Drugs. 2000 Aug;60(2):447-79.
规格 10mg