| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
BMS-929075 primarily targets the HCV NS5B replicase, which is the RNA-dependent RNA polymerase essential for HCV replication. It binds to an allosteric site on the palm domain of the NS5B enzyme, inhibiting its polymerase activity. This prevents the replication of the HCV genome. BMS-929075 is a potent and orally active inhibitor with high oral bioavailability.
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| ln Vitro |
With CC50 values of 60, >12.5, and >50 µM for Huh-7, HepG2, and primary human liver, respectively, BMS-929075 (0-60 µM) exhibits cytotoxicity [1].
In vitro, BMS-929075 is a potent inhibitor of HCV NS5B replicase. It has demonstrated efficacy in a triple combination regimen in HCV replicon cells. Its activity is assessed by measuring its ability to inhibit HCV replication in cell-based replicon assays. The compound exhibits a favorable cytotoxicity window. Specific IC50 values are not detailed in the provided search results. |
| ln Vivo |
In terms of pharmacokinetic characteristics, BMS-929075 (compound 37) (2 mg/kg intravenously; 6 mg/kg bucally) demonstrated good results, with a bridge bioavailability of 48% [1].
In vivo, BMS-929075 is an orally active compound with high oral bioavailability. It has been advanced to Phase 1 clinical studies for the treatment of HCV infection. Its favorable pharmacokinetic parameters across preclinical animal species support its development as an oral antiviral agent. Further studies are needed to fully characterize its in vivo efficacy and safety in clinical trials. |
| Enzyme Assay |
The in vitro activity of BMS-929075 is assessed using cell-based HCV replicon assays. Huh-7 cells harboring HCV replicons are treated with varying concentrations of BMS-929075. HCV replication is assessed by measuring HCV RNA levels by qPCR or by measuring reporter gene activity. The IC50 is determined from dose-response curves. The compound's cytotoxicity is assessed using standard cell viability assays.
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| Cell Assay |
For cellular assays, Huh-7 cells harboring HCV replicons are cultured in appropriate media. Cells are treated with various concentrations of BMS-929075 (typically 0.1-1000 nM) for defined periods. HCV RNA levels are measured by qPCR. Cell viability is assessed using MTT or CellTiter-Glo assays. The combination of BMS-929075 with other HCV inhibitors can be assessed in replicon assays.
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| Animal Protocol |
In vivo, BMS-929075 is typically administered orally to animal models or patients. In preclinical studies, the compound is administered at various doses, and pharmacokinetic parameters are assessed. In clinical trials, the compound is administered to patients with HCV infection, and efficacy is assessed by measuring HCV RNA levels in plasma. Pharmacokinetic studies involve measuring BMS-929075 levels in plasma.
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| ADME/Pharmacokinetics |
BMS-929075 has a molecular weight of approximately 475.5 g/mol. It is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. The compound should be stored as a powder at -20°C under desiccated conditions. Specific solubility and pharmacokinetic parameters are not detailed in the provided search results. It has high oral bioavailability.
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| Toxicity/Toxicokinetics |
BMS-929075 shows cytotoxicity. The compound is intended for clinical use under appropriate regulatory oversight. Comprehensive toxicological studies are required to establish its full safety profile. Standard laboratory safety precautions should be followed when handling the compound. Its safety and efficacy are being evaluated in clinical trials.
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| References | |
| Additional Infomation |
BMS-929075 is being investigated in the clinical trial NCT01525212 (a multiple escalation study of BMS-929075 in patients infected with hepatitis C virus (HCV)).
BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. It shows high oral bioavailability. BMS-929075 has been advanced to Phase 1 clinical studies for the treatment of hepatitis C virus (HCV) infection. It has demonstrated efficacy in a triple combination regimen in HCV replicon cells. The compound is not approved for clinical use and is intended for research purposes. |
| Molecular Formula |
C31H24F2N4O3
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|---|---|
| Molecular Weight |
538.5548
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| Exact Mass |
538.181
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| CAS # |
1217338-97-0
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| PubChem CID |
59275404
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
725.5±60.0 °C at 760 mmHg
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| Flash Point |
392.6±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
3.93
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
920
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C2C(C(NC)=O)=C(C3C=CC(=CC=3)F)OC=2C=CC=1C1=C(C)C=CC(=C1)C(NC1(C2N=CC=CN=2)CC1)=O
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| InChi Key |
LZAUGCMVNLZVJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H24F2N4O3/c1-17-4-5-19(28(38)37-31(12-13-31)30-35-14-3-15-36-30)16-22(17)21-10-11-23-24(26(21)33)25(29(39)34-2)27(40-23)18-6-8-20(32)9-7-18/h3-11,14-16H,12-13H2,1-2H3,(H,34,39)(H,37,38)
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| Chemical Name |
4-fluoro-2-(4-fluorophenyl)-N-methyl-5-[2-methyl-5-[(1-pyrimidin-2-ylcyclopropyl)carbamoyl]phenyl]-1-benzofuran-3-carboxamide
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| Synonyms |
BMS929075; BMS 929075; BMS-929075
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8568 mL | 9.2842 mL | 18.5684 mL | |
| 5 mM | 0.3714 mL | 1.8568 mL | 3.7137 mL | |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8568 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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