Tenofovir exalidex CMX-157|cas:911208-73-6|西域试剂

Tenofovir exalidex CMX-157

产品编号：Bellancom-109014| CAS NO：911208-73-6| 分子式：C₂₈H₅₂N₅O₅P| 分子量：569.72

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-109014	￥805.00	杭州北京（现货）
Bellancom-109014	￥1190.00	杭州北京（现货）
Bellancom-109014	￥2310.00	杭州北京（现货）
Bellancom-109014	￥3500.00	杭州北京（现货）
Bellancom-109014	￥5250.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Tenofovir exalidex CMX-157

产品介绍

Tenofovir exalidex (CMX157) 是一种非环核苷酸类似物 Tenofovir 的脂质结合物，对野生型和抗逆转录病毒耐药的 HIV 毒株，包括多药核苷/核苷酸类似物耐药病毒，都有活性。Tenofovir exalidex 对人外周血单个核细胞中所有主要的HIV-1和HIV-2亚型以及单核细胞来源的巨噬细胞中所有 HIV-1 菌株具有活性，EC₅₀ 范围在 0.2 和 7.2 nM 之间。Tenofovir exalidex 具有口服活性，无明显毒性。Tenofovir exalidex 对 HBV 也有活性。

生物活性

Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC₅₀s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.

体外研究

Tenofovir exalidex is consistently >300-fold more active than Tenofovir against multiple viruses in several different cell systems. Tenofovir exalidex will be effective against MNR mutants, including those that are unresponsive to all currently available NRTIs. Notably, the average EC₅₀ in PBMCs for CMX157 against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O was 2.6 nM (range, 0.2 to 7.2 nM).
Tenofovir exalidex exerts its therapeutic actions by inhibiting HBV polymerase-mediated HBV DNA elongation, but there is no known binding of cyclophilins to HBV polymerase nor participation of cyclophilins in DNA elongation. The combinational effect of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) on HBV DNA production is more consistent with the two compounds acting on distinct steps of the HBV life cycle.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Tenofovir exalidex (Sprague-Dawley rats) is orally available and has no apparent toxicity when given orally to rats for 7 days at doses of 10, 30, or 100 mg/kg/day. Tenofovir exalidex (5-10 mg/kg; oral gavage; daily for a period of 16 days) decreases liver HBV DNA levels dose-dependently.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female transgenic mice HBV transgenic Tg05 mice (C57BL/6)
Dosage:	5 mg/kg, 10 mg/kg
Administration:	Oral gavage; daily for a period of 16 days
Result:	The reductions in HBV DNA were 55% and 97% for low-dose (5 mg/kg/day) and high-dose (10 mg/kg/day), respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female transgenic mice HBV transgenic Tg05 mice (C57BL/6)
Dosage:	5 mg/kg, 10 mg/kg
Administration:	Oral gavage; daily for a period of 16 days
Result:	The reductions in HBV DNA were 55% and 97% for low-dose (5 mg/kg/day) and high-dose (10 mg/kg/day), respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (175.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7552 mL	8.7762 mL	17.5525 mL
5 mM	0.3510 mL	1.7552 mL	3.5105 mL
10 mM	0.1755 mL	0.8776 mL	1.7552 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (3.51 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。