| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
HMG-CoA reductase (HMGCR).
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|---|---|
| ln Vitro |
Bemfivastatin hemicalcium is an HMG-CoA reductase inhibitor that enhances the activity of liver extracts, indicating its effectiveness in reducing cholesterol synthesis in hepatocytes. It reduces blood lipid levels and is used in research for hypercholesterolemia. It may also be studied in the context of statin-related hypercholesterolemic myalgia in statin-intolerant patients.
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| Enzyme Assay |
The HMG-CoA reductase inhibition assay is performed using recombinant human HMG-CoA reductase enzyme. The assay mixture contains the compound, enzyme, and the substrate HMG-CoA, along with NADPH as a cofactor. After incubation, the reaction is stopped, and the formation of mevalonate (the product) is quantified by LC-MS/MS or a spectrophotometric method. The IC50 value is calculated from the inhibition curve.
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| Cell Assay |
For cellular activity, primary human hepatocytes or HepG2 cells are treated with Bemfivastatin hemicalcium. Cholesterol synthesis is measured by incorporating 14C-acetate or 3H-water into sterols. Cells are incubated with the compound and labeled precursor, followed by lipid extraction and scintillation counting. Effects on LDL receptor expression and uptake are assessed by Western blot and fluorescent LDL uptake assays.
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| Animal Protocol |
In vivo lipid-lowering activity is typically assessed in hyperlipidemic rodent models (e.g., high-fat diet-fed rats or hamsters). Animals are dosed orally with Bemfivastatin hemicalcium daily for 1-2 weeks. Serum lipid profiles (total cholesterol, LDL cholesterol, triglycerides) are measured at baseline and after treatment. Liver HMG-CoA reductase activity and hepatic cholesterol content are also evaluated.
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| ADME/Pharmacokinetics |
As an orally active statin, Bemfivastatin hemicalcium is absorbed from the gastrointestinal tract, undergoes extensive first-pass extraction by the liver (the target organ), and is primarily eliminated via the biliary route. Its plasma half-life is relatively short due to rapid hepatic uptake. Detailed PK parameters are available in proprietary preclinical reports.
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| Toxicity/Toxicokinetics |
No-observed-adverse-effect levels (NOAELs) in preclinical studies are: ≥320 mg/kg/day for developmental toxicity in rats, ≥12.5 mg/kg/day for maternal toxicity in rabbits, and ≥25 mg/kg/day for developmental toxicity in rabbits. As a statin, potential adverse effects include hepatotoxicity, myopathy, and elevated liver enzymes, though the hemicalcium salt may improve tolerability.
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| References | |
| Additional Infomation |
Bemfivastatin hemicalcium is an investigational drug candidate, not an approved drug. Its development likely focuses on patients who are statin-intolerant (experience myalgia with standard statins). The hemicalcium salt formulation may offer advantages in terms of solubility, stability, or reduced adverse effects compared to the parent compound. It is also known as PPD 10558.
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| Molecular Formula |
C68H72CAF2N4O12
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|---|---|
| Molecular Weight |
1215.39370536804
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| Exact Mass |
1214.474
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| CAS # |
805241-64-9
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| Related CAS # |
Bemfivastatin;805241-79-6
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| PubChem CID |
11959785
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
87
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| Complexity |
863
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C1=C(C(=C(N1CC[C@H](C[C@H](CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=C(C=C4)CO.CC(C)C1=C(C(=C(N1CC[C@H](C[C@H](CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=C(C=C4)CO.[Ca+2]
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| InChi Key |
DPHJMDHNVYEKRX-GWQGKXOTSA-L
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| InChi Code |
InChI=1S/2C34H37FN2O6.Ca/c2*1-21(2)32-31(34(43)36-26-14-8-22(20-38)9-15-26)30(23-6-4-3-5-7-23)33(24-10-12-25(35)13-11-24)37(32)17-16-27(39)18-28(40)19-29(41)42;/h2*3-15,21,27-28,38-40H,16-20H2,1-2H3,(H,36,43)(H,41,42);/q;;+2/p-2/t2*27-,28-;/m11./s1
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| Chemical Name |
calcium;(3R,5R)-7-[2-(4-fluorophenyl)-4-[[4-(hydroxymethyl)phenyl]carbamoyl]-3-phenyl-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 0.8228 mL | 4.1139 mL | 8.2278 mL | |
| 5 mM | 0.1646 mL | 0.8228 mL | 1.6456 mL | |
| 10 mM | 0.0823 mL | 0.4114 mL | 0.8228 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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