TC14012 acetate 是 T140 的血清稳定衍生物，是一种选择性的肽模拟 CXCR4 拮抗剂，IC50 为 19.3 nM。 TC14012 还是一种有效的 CXCR7 激动剂，EC50 为 350 nM，可将 β-arrestin 2 募集到 CXCR7。 TC14012 具有抗癌活性和抗 HIV 活性。

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

TC14012 (1 mM) inhibits more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain. TC14012 (1 mM) does not inhibit all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain. TC14012 leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4. CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin upon stimulation with TC14012 whereas CXCR4 and CXCR4-Cter7 remain silent.

TP2112L

C92H144N34O21S2

2126.47

TC14012 acetate(368874-34-4 free base)

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years