| Cas No.: | 144217-65-2 |
| Synonyms: | YYA 021; YYA021 |
| SMILES: | O=C(NC1=CC=C(C)C=C1)C(NC2CC(C)(C)NC(C)(C)C2)=O |
| Formula: | C18H27N3O2 |
| M.Wt: | 317.43 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity. YYA-021 is determined by a single round assay using cYTA48P virus and TZM-bl cells. YYA-021 is broadly distributed in tissues, probably as a result of its hydrophobicity. The plasma concentrations of YYA-021 in both species remained at micromolar levels for several hours post-injection. [1] YYA-021 also enhances the neutralizing activity of KD-247 against simian-human immunodeficiency virus (SHIV)-KS661 strain via highly synergistic interactions. YYA-021 might have promise as a lead compound for the intravenous administration in a cocktail therapy with anti-gp120 monoclonal antibodies such as KD-247 and with co-receptor antagonists such as T140. [2] |
| Target: | IC50 value: 8.4 μM Target: HIV |
| References: | [1]. Mizuguchi T, et al. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor. Bioorg Med Chem Lett. 2016 Jan 15;26(2):397-400. [2]. Hashimoto C, et al. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics. Bioorg Med Chem. 2013 Dec 15;21(24):7884-9. |

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