YYA-021 |
| Katalog-Nr.GC12606 |
YYA-021 ist ein niedermolekulares CD4-Mimetikum, das den HIV-Eintritt hemmt, mit hoher Anti-HIV-AktivitÄt und geringer ZytotoxizitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 144217-65-2
Sample solution is provided at 25 µL, 10mM.
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YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry [1].
CD4 is a cell surface protein. The entry of human immunodeficiency virus type 1 (HIV-1) into target cells is initiated by the interaction of CD4 and viral envelope glycoprotein gp120. CD4 mimic inhibits the interaction between gp120 and CD4 and then inhibits HIV entry [1].
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry. YYA-021 competitively inhibited gp120-CD4 interaction [1]. 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 [2].
In Jcl:SD rats, the maximum tolerated dose of YYA-021.HCl was 2.5 mg. When administrated by tail vein injection, YYA-021 exhibited widespread tissue distribution due to its hydrophobicity. In a rhesus macaque, the maximum tolerated dose of YYA-021.HCl was 35.3 mg [1].
References:
[1]. Hashimoto C, Narumi T, Otsuki H, et al. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics. Bioorg Med Chem, 2013, 21(24): 7884-7889.
[2]. Otsuki H, Hishiki T, Miura T, et al. Generation of a replication-competent simian-human immunodeficiency virus, the neutralization sensitivity of which can be enhanced in the presence of a small-molecule CD4 mimic. J Gen Virol, 2013, 94(Pt 12): 2710-2716.
| Cas No. | 144217-65-2 | SDF | |
| Canonical SMILES | CC1=CC=C(C=C1)NC(=O)C(=O)NC2CC(NC(C2)(C)C)(C)C | ||
| Formula | C18 H27 N3 O2 | M.Wt | 317.43 |
| Löslichkeit | DMF: 12 mg/ml,DMF:PBS (pH7.2) (1:30): 0.03 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.125 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1503 mL | 15.7515 mL | 31.503 mL |
| 5 mM | 630.1 μL | 3.1503 mL | 6.3006 mL |
| 10 mM | 315 μL | 1.5752 mL | 3.1503 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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