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Purity: ≥98%
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.
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| 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 Formula |
C18H27N3O2
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| Molecular Weight |
317.43
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| CAS # |
144217-65-2
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| Related CAS # |
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| SMILES |
O=C(NC1=CC=C(C)C=C1)C(NC2CC(C)(C)NC(C)(C)C2)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1503 mL | 15.7515 mL | 31.5030 mL | |
| 5 mM | 0.6301 mL | 3.1503 mL | 6.3006 mL | |
| 10 mM | 0.3150 mL | 1.5752 mL | 3.1503 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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