TAK-779 was the first non-peptide antagonist for C-C chemokine receptor type 5 (CCR5) receptor that effectively blocks the cell entry of R5-type HIV [1]. TAK-779 is also an antagonist of CCR2b and CXC chemokine receptor 3 (CXCR3) [2]. Treatment with TAK-779 reduced incidence and severity of experimental autoimmune encephalomyelitis due to reduced migration of inflammatory cells into the CNS [3].
Technical information:
Chemical Formula: | C33H39N2O2.Cl | |
CAS #: | 229005-80-5 | |
Molecular Weight: | 531.14 | |
Purity: | > 98% | |
Appearance: | Off-white | |
Chemical Name: | 1-(4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol | |
Solubility: | Up to 37 mM in DMSO | |
Synonyms: | Takeda 779, TAK 779, TAK779 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
1. | Baba M, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. 1999; 96(10): 5698-5703 Pubmed ID: 10318947 |
2. | Gao P, et al. The unique target specificity of a nonpeptide chemokine receptor antagonist: Selective blockade of two Th1 chemokine receptors CCR5 and CXCR3. J Leukoc Biol 2003; 73(2): 273-280 Pubmed ID: 12554804 |
3. | Kim MB, et al. CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV. Expert Opin Investig Drugs. 2016; 25(12): 13771392. Pubmed ID: 27791451 |
4. | Ni J, et al. The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function. Br J Pharmacol 2009; 158(8):2046-56. Pubmed ID: 12554804 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.