144217-65-2

144217-65-2 structure

Name: YYA-021
Chemical Name: yya-021
CAS Number: 144217-65-2
Molecular Formula: C₁₈H₂₇N₃O₂
Molecular Weight: 317.42600
Catalog: Signaling Pathways Anti-infection HIV
Create Date: 2016-07-12 14:37:28
Modify Date: 2024-01-14 18:44:41
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity. IC50 value: 8.4 μM Target: HIVIC50 (=8.4 μM) value of 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]

Name	yya-021
Synonyms	N-(2,2,6,6-Tetramethyl-piperidin-4-yl)-N'-p-tolyl-oxalamide

Description	YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity. IC50 value: 8.4 μM Target: HIVIC50 (=8.4 μM) value of 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]
Related Catalog	Signaling Pathways >> Anti-infection >> HIV Research Areas >> Infection
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.