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| Size | Price | Stock |
|---|---|---|
| 5mg | $65 | 3-6 Days |
| 10mg | $95 | 3-6 Days |
| 25mg | $145 | 3-6 Days |
| 50mg | $209 | 3-6 Days |
| 100mg | $339 | 3-6 Days |
| 250mg | $650 | 3-6 Days |
| 500mg | $1020 | 3-6 Days |
: Cat #: V1840 CAS #: 144217-65-2 Purity ≥ 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.
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| Molecular Weight (MW) | 317.43 |
|---|---|
| Molecular 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 | O=C(NC1CC(C)(C)NC(C)(C)C1)C(NC2=CC=C(C)C=C2)=O |
| Synonyms | YYA-021; YYA 021; YYA021 |
| Protocol | 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 Vivo | Rats and rhesus macaques | |
| Animal model | Rat, dog and monkey |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.1503 mL | 15.7515 mL | 31.5030 mL | 63.0060 mL |
| 5mM | 0.6301 mL | 3.1503 mL | 6.3006 mL | 12.6012 mL |
| 10mM | 0.3150 mL | 1.5752 mL | 3.1503 mL | 6.3006 mL |
| 20mM | 0.1575 mL | 0.7876 mL | 1.5752 mL | 3.1503 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.