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TAK-779

Chemical Structure : TAK-779

CAS No.: 229005-80-5

TAK-779 (TAK779;TAK 799;Takeda 779)

货号: PC-43512Not For Human Use, Lab Use Only.

TAK-779 is a potent, specific, nonpeptide CCR5 antagonist with Kd of 0.45 nM, antagonizes CCR2b to a lesser extent (27 nM) but does not affect CCR1, CCR3, or CCR4.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAK-779 is a potent, specific, nonpeptide CCR5 antagonist with Kd of 0.45 nM, antagonizes CCR2b to a lesser extent (27 nM) but does not affect CCR1, CCR3, or CCR4.
TAK-779 also blocks the binding of macrophage inflammatory protein 1α and macrophage inflammatory protein 1β to the cells with an IC50 of 1.0 nM.
TAK-779 TAK-779 displays highly potent and selective inhibition of the replication of macrophage (M)-tropic HIV-1 (Ba-L strain) in both MAGI-CCR5 cells and PBMCs with EC50 of 1.2 and 3.7 nM, respectively.

物理化学性质&存储条件

分子量
分子式 C33H39ClN2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 27 mg/mL

Chemical Name/SMILES

2H-Pyran-4-aminium, N-[[4-[[[6,7-dihydro-2-(4-methylphenyl)-5H-benzocyclohepten-8-yl]carbonyl]amino]phenyl]methyl]tetrahydro-N,N-dimethyl-, chloride (1:1)

参考文献

1. Baba M, Nishimura O, et al. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5698-703.

2. Shiraishi M, et al. J Med Chem. 2000 May 18;43(10):2049-63.

3. Gorry PR, et al. J Virol. 2002 Jun;76(12):6277-92.

4. Nedjai B, et al. Br J Pharmacol. 2015 Apr;172(7):1822-33.

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