product name YYA-021
Description: YYA-021 is a small-molecule CD4-mimic HIV entry inhibitor that competitively inhibits the interaction between gp120 and CD4. 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.
References: J Gen Virol. 2013 Dec;94(Pt 12):2710-6; Bioorg Med Chem. 2013 Dec 15;21(24):7884-9.
317.43
Formula
C18H27N3O2
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)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423565
| 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: Cell Assay: |
|---|---|
| In Vivo | Rats and rhesus macaques |
| Animal model | Rat, dog and monkey |
| Formulation & Dosage | 14 mg/kg (rats), 13.4 mg/kg (rhesus macaques); i.v. injection |
| References | J Gen Virol. 2013 Dec;94(Pt 12):2710-6; Bioorg Med Chem. 2013 Dec 15;21(24):7884-9. |
