BMS-818251
Based on 1 Customer Validation
BMS-818251 is a HIV-1 attachment and entry inhibitor. BMS-818251 binds to HIV-1 Env gp120, interferes with viral attachment and entry processes, and inhibits HIV-1 viral replication. BMS-818251 can be used in studies related to HIV-1 infection.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.36%
- No. CAS: 2974489-09-1
- Fòrmula: C29H26N6O5S
- Peso molecular:570.62
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
HIV-1 |
In Vitro
BMS-818251 (administered 1 h before infection at 12.5-20 nM) identifies single-amino-acid mutations on the HIV-1 BG505 envelope protein. These mutations cluster around the binding site of BMS-818251 and confer viral resistance to BMS-818251[1].
BMS-818251 (serial dilution starting from 20 μM; 2 days) potently inhibits the entry of HIV-1 NL4-3 pseudovirus into TZM-bl cells, with an EC50 of 0.019 nM[2].
BMS-818251 (serial dilution starting from 20 μM; 2 days) potently neutralizes a panel of 30 cross-subtype HIV-1 primary isolates in TZM-bl cells, with a geometric mean IC50 of approximately 0.002 μM[2].
BMS-818251 (serial dilution starting from 20 μM; 2 days) potently neutralizes a panel of 208 HIV-1 isolates spanning multiple subtype clades in TZM-bl cells, with a geometric mean IC50 of 0.0015 μM and a median IC50 of 0.0005 μM[2].
BMS-818251 binds to purified BG505 DS-SOSIP.664 HIV-1 Env trimer at 37 °C with an affinity of 0.047 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 2974489-09-1
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Appearance Solid
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Peso molecular 570.62
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Fòrmula C29H26N6O5S
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Color White to off-white
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SMILES
N#C/C(C1=CC=CC=C1)=C2CCN(CC/2)C(C(C3=CNC4=C(C5=CSC(C(NCCO)=O)=N5)N=CC(OC)=C34)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (175.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.76 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lai Y-T, et al. Fostemsavir analog BMS-818251 has enhanced viral neutralization potency and similar escape mutation profile. Antimicrob Agents Chemother. 2025;69(10):e0191024. [Content Brief]
[2]. Lai YT, et al. Lattice engineering enables definition of molecular features allowing for potent small-molecule inhibition of HIV-1 entry. Nat Commun. 2019;10(1):47. Published 2019 Jan 3. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7525 mL | 8.7624 mL | 17.5248 mL | 43.8120 mL |
| 5 mM | 0.3505 mL | 1.7525 mL | 3.5050 mL | 8.7624 mL | |
| 10 mM | 0.1752 mL | 0.8762 mL | 1.7525 mL | 4.3812 mL | |
| 15 mM | 0.1168 mL | 0.5842 mL | 1.1683 mL | 2.9208 mL | |
| 20 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1906 mL | |
| 25 mM | 0.0701 mL | 0.3505 mL | 0.7010 mL | 1.7525 mL | |
| 30 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4604 mL | |
| 40 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL | |
| 50 mM | 0.0350 mL | 0.1752 mL | 0.3505 mL | 0.8762 mL | |
| 60 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7302 mL | |
| 80 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5476 mL | |
| 100 mM | 0.0175 mL | 0.0876 mL | 0.1752 mL | 0.4381 mL |
BMS-818251 Related Classifications
HY-125183 Related Classifications
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