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    InvivoChem Cat #: V1840
    CAS #: 144217-65-2Purity ≥98%

    Description: YYA-021 is a novel and potent small-molecule CD4-mimic agent that acts as an HIV entry inhibitor by competitively inhibiting the interaction between an HIV-1 envelope glycoprotein gp120 and a cellular surface protein CD4. It has relatively high potency and low cytotoxicity. In TZM-bl cells infected with simian-human immunodeficiency virus isolate MNA (SHIV MNA) or HIV-1 MNA pseudotyped viruses, YYA-021 inhibited the entry of Envs of SHIV MNA and HIV-1. KD-247 (the anti-V3 loop mAb, 50 μg) caused 50% neutralization of HIV-1 MNA. However, in the presence of 20 μM of YYA-021, KD-247 (<0.05 μg) caused 50% neutralization of HIV-1 MNA, which suggested that the synergistic neutralization effect of YYA-021 and KD-247. In the presence of YYA-021, SHIV MNA became more sensitive to IgG. YYA-021 might have promise for intravenous administration when used combinatorially with anti-gp120 monoclonal antibodies.

    References: J Gen Virol. 2013 Dec;94(Pt 12):2710-6; Bioorg Med Chem. 2013 Dec 15;21(24):7884-9.

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    Molecular Weight (MW)317.43
    CAS No.144217-65-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:<1 mg/mL
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo) O=C(NC1CC(C)(C)NC(C)(C)C1)C(NC2=CC=C(C)C=C2)=O
    Synonyms YYA-021; YYA 021; YYA021

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    In Vitro

    In vitro activity: YYA-021 enhances the neutralization sensitivity of simian-human immunodeficiency virus (SHIV) carrying the envelope from the clade B clinical human immunodeficiency virus type 1 (HIV-1) isolate MNA. 

    Kinase Assay: 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 

    Cell Assay: HIV IC50 (=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.

    In VivoRats and rhesus macaques
    Animal modelRat, dog and monkey
    Formulation & Dosage14 mg/kg (rats), 13.4 mg/kg (rhesus macaques); i.v. injection
    ReferencesJ Gen Virol. 2013 Dec;94(Pt 12):2710-6; Bioorg Med Chem. 2013 Dec 15;21(24):7884-9.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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