Aplaviroc hydrochloride AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride|cas:461023-63-2|西域试剂

Aplaviroc hydrochloride AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride,99.76%

产品编号：Bellancom-17450A| CAS NO：461023-63-2| 分子式：C₃₃H₄₄ClN₃O₆| 分子量：614.17

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货号	价格	库存与货期
Bellancom-17450A	￥5800.00	杭州北京（现货）
Bellancom-17450A	￥9500.00	杭州北京（现货）
Bellancom-17450A	￥16500.00	杭州北京（现货）
Bellancom-17450A	￥34500.00	杭州北京（现货）

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Aplaviroc hydrochloride AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride

产品介绍

Aplaviroc (AK 602) hydrochloride，SDP的一个衍生物，是 CCR5 的拮抗剂，其对 HIV-1_Ba-L， HIV-1_JRFL 和 HIV-1_MOKW 的 IC₅₀ 值为 0.1-0.4 nM。

生物活性

Aplaviroc (AK 602) hydrochloride, a SDP derivative, is a CCR5 antagonist, with IC₅₀s of 0.1-0.4 nM for HIV-1_Ba-L, HIV-1_JRFL and HIV-1_MOKW.

体外研究

Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1_Ba-L, HIV-1_JRFL and HIV-1_MOKW) with IC₅₀ values of 0.1 to 0.4 nM. Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. Aplaviroc suppresses the infectivity and replication of two HIV-1_MDR variants, HIV-1_MM and HIV-1_JSL, at extremely low concentrations (IC₅₀ values of 0.4 to 0.6 nM). Aplaviroc binds to CCR5 with high affinity. The K_d values thus determined for Aplaviroc, E913, E921/TAK-779, and AK671/SCH-C are 2.9±1.0, 111.7±3.5, 32.2±9.6, and 16.0±1.5 nM, respectively. Aplaviroc potently blocks rgp120/sCD4 binding to CCR5 with an IC₅₀ value of 2.7 nM. These results suggest that the potent activity of Aplaviroc against R5 HIV-1 stems from its binding to ECL2B and/or its vicinity with high affinity, resulting in inhibition of gp120/CD4 binding to CCR5.

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

体内研究

The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly.
Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice.

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

Animal Model:	hu-PBMC-NOG mice.
Dosage:	60 mg/kg.
Administration:	Single intraperitoneal administration, bid, daily.
Result:	The numbers of CD4⁺ cells/μL in saline-treated mice were significantly less than those of AK602-treated, ddI-treated, or uninfected mice.

体内研究

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

Animal Model:	hu-PBMC-NOG mice.
Dosage:	60 mg/kg.
Administration:	Single intraperitoneal administration, bid, daily.
Result:	The numbers of CD4⁺ cells/μL in saline-treated mice were significantly less than those of AK602-treated, ddI-treated, or uninfected mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (325.64 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6282 mL	8.1411 mL	16.2821 mL
5 mM	0.3256 mL	1.6282 mL	3.2564 mL
10 mM	0.1628 mL	0.8141 mL	1.6282 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 (sealed storage, away from moisture)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

此方案可获得 ≥ 12.5 mg/mL (20.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 125.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

此方案可获得 ≥ 12.5 mg/mL (20.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 125.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

此方案可获得 ≥ 12.5 mg/mL (20.35 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 125.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。