TAK-779 is a potent and selective nonpeptide antagonist ofCCR5andCXCR3, with aK_iof 1.1 nM forCCR5, and effectively and selectively inhibitsR5HIV-1, withEC₅₀andEC₉₀of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a K_iof 1.1 nM, and effectively and selectively inhibits R5 HIV-1, with EC₅₀and EC₉₀of 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 IC₅₀for CCR2b of 27 nM. TAK-779 also completely inhibits the binding of [¹²⁵I]-RANTES to CHO/CCR5 cells with an IC₅₀of 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^[1]. TAK-779 is an antagonist of CXCR3, and inhibits the migration of T cells but not T cell proliferation^[2].

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)^[2]. 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)^[3].

531.13

Solid

C₃₃H₃₉ClN₂O₂

229005-80-5

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : ≥ 25 mg/mL(47.07 mM)

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

*"≥" means soluble, but saturation unknown.

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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-CDin 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 μL20% 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。