TAK-779 Takeda 779|cas:229005-80-5|西域试剂

TAK-779 Takeda 779,99.72%

产品编号：Bellancom-13406| CAS NO：229005-80-5| 分子式：C₃₃H₃₉ClN₂O₂| 分子量：531.13

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货号	价格	库存与货期
Bellancom-13406	￥990.00	杭州北京（现货）
Bellancom-13406	￥1580.00	杭州北京（现货）
Bellancom-13406	￥4750.00	杭州北京（现货）
Bellancom-13406	￥7600.00	杭州北京（现货）

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TAK-779 Takeda 779

产品介绍

TAK-779 是一种有效的，选择性的，非肽类 CCR5 和 CXCR3 拮抗剂，对 CCR5 的 K_i 值为 1.1 nM，同时可以有效地，选择性地抑制 R5 HIV-1，在 MAGI-CCR5 细胞中，EC₅₀ 和 EC₉₀ 值分别为 1.2 nM 和 5.7 nM。

生物活性

TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a K_i of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC₅₀ and EC₉₀ of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

体外研究

TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a K_i of 1.1 nM, and effectively and selectively inhibits R5 HIV-1, with EC₅₀ and EC₉₀ of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. TAK-779 less potently blocks the binding of [¹²⁵I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells, with an IC₅₀ for CCR2b of 27 nM. TAK-779 also completely inhibits the binding of [¹²⁵I]-RANTES to CHO/CCR5 cells with an IC₅₀ of 1.4 nM. TAK-779 (20 nM) selectively inhibits CCR5-mediated Ca²⁺-signaling. In addition, TAK-779 shows no inhibition on X4 HIV-1 strains. TAK-779 is an antagonist of CXCR3, and inhibits the migration of T cells but not T cell proliferation.

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

体内研究

TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. TAK-779 also decreases the number of CD4⁺ as well as CD8⁺ T cells in spleen, blood and recipient mesenteric lymph nodes (MLN). TAK-779 (150 µg per mouse, s.c.) supppresses the development of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoprotein (MOG)-immunized C57BL/6 mice. TAK-779 decreases the infiltration of CXCR3 and CCR5 bearing leukocytes into the spinal cord. TAK-779 does not alter myelin oligodendrocyte glycoprotein (MOG)-specific immune responses or affect the potential of MOG-specific T cells to transfer experimental autoimmune encephalomyelitis (EAE).

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 25 mg/mL (47.07 mM)

H₂O : 16.66 mg/mL (31.37 mM; Need ultrasonic and warming)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8828 mL	9.4139 mL	18.8278 mL
5 mM	0.3766 mL	1.8828 mL	3.7656 mL
10 mM	0.1883 mL	0.9414 mL	1.8828 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： PBS
Solubility: 50 mg/mL (94.14 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.58 mg/mL (4.86 mM); Clear solution

此方案可获得 ≥ 2.58 mg/mL (4.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.58 mg/mL (4.86 mM); Clear solution

此方案可获得 ≥ 2.58 mg/mL (4.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.8 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.58 mg/mL (4.86 mM); Clear solution

此方案可获得 ≥ 2.58 mg/mL (4.86 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 25.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。