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TAK-779
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TAK-779图片
CAS NO:229005-80-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
Takeda 779
产品介绍
TAK-779 是一种有效的,选择性的,非肽类CCR5CXCR3拮抗剂,对CCR5Ki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,EC50EC90值分别为 1.2 nM 和 5.7 nM。
生物活性

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

IC50& Target[1][4]

MIP-1α-CCR5

1 nM (IC50, in CHO/CCR5 cells)

MIP-1β-CCR5

1 nM (IC50, in CHO/CCR5 cells)

RANTES-CCR5

1.4 nM (IC50, in CHO/CCR5 cells)

MCP-1-CCR2b

27 nM (IC50, in CHO/CCR5 cells)

R5 HIV-1 (Ba-L)

1.2 nM (EC50, in MAGI-CCR5 cells)

R5 HIV-1 (Ba-L)

5.7 nM (EC90, in MAGI-CCR5 cells)

R5 HIV-1 (Ba-L)

3.7 nM (EC50, in PBMCs)

R5 HIV-1 (Ba-L)

12.8 nM (EC90, in PBMCs)

R5 HIV-1 (KK)

1.6 nM (EC50, in PBMCs)

R5 HIV-1 (KK)

20.8 nM (EC90, in PBMCs)

R5 HIV-1 (HHA)

3.2 nM (EC50, in PBMCs)

R5 HIV-1 (HHA)

7.5 nM (EC90, in PBMCs)

R5 HIV-1 (CTV)

3.5 nM (EC50, in PBMCs)

R5 HIV-1 (CTV)

27 nM (EC90, in PBMCs)

mCXCR3

369 nM (IC50, in PBMCs)

体外研究
(In Vitro)

TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Kiof 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].

体内研究
(In Vivo)

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].

分子量

531.13

性状

Solid

Formula

C33H39ClN2O2

CAS 号

229005-80-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

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 mg5 mg10 mg
1 mM1.8828 mL9.4139 mL18.8278 mL
5 mM0.3766 mL1.8828 mL3.7656 mL
10 mM0.1883 mL0.9414 mL1.8828 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℃, 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。

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-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。

*以上所有助溶剂都可在本网站选购。