| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
HMG-CoA reductase (HMGCR). As a statin, PPD 10558 inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis. This leads to decreased hepatic cholesterol production, upregulation of LDL receptors, and increased clearance of circulating LDL cholesterol.
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| ln Vitro |
PPD 10558 inhibits HMG-CoA reductase activity in enzymatic assays. As a statin, it reduces cholesterol synthesis in hepatic cell lines. The compound enhances the activity of liver extraction. In vitro studies demonstrate inhibition of cholesterol biosynthesis in cultured hepatocytes. The compound shows potency comparable to other statins in enzyme inhibition assays. Its effects on cellular cholesterol metabolism, including LDL receptor upregulation, have been characterized in liver cell models.
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| ln Vivo |
PPD 10558 demonstrates lipid-lowering activity in animal models of hypercholesterolemia. As an orally active statin, it reduces total cholesterol, LDL cholesterol, and triglyceride levels in circulation. The compound enhances hepatic extraction of lipoproteins. In developmental toxicity studies, daily oral administration to pregnant rats and rabbits during organogenesis showed little toxic effect on development, with a NOAEL of ≥320 mg/kg.
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| Enzyme Assay |
HMG-CoA reductase enzyme inhibition assays are performed using recombinant human HMG-CoA reductase expressed in E. coli or mammalian systems. The enzyme is incubated with the substrate HMG-CoA and [14C]-labeled or [3H]-labeled cofactor NADPH in assay buffer (50 mM KH2PO4 pH 7.4, 0.1 M KCl, 1 mM EDTA, 5 mM DTT). The reaction is incubated at 37°C for 30-60 minutes. The product mevalonate is separated from substrate by TLC or solid-phase extraction and quantified by scintillation counting. Test compounds are serially diluted and added to the reaction mixture. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate.
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| Cell Assay |
Cellular activity is evaluated in hepatic cell lines (e.g., HepG2, primary human hepatocytes). Cells are cultured in DMEM with 10% FBS and treated with PPD 10558 at various concentrations (0.001-10 μM) for 24-72 hours. Cholesterol biosynthesis is measured by incorporation of [14C]-acetate or [3H]-water into sterols. LDL receptor protein levels are measured by Western blotting or flow cytometry. Intracellular cholesterol content is quantified using enzymatic assays. Cell viability is assessed using MTT or CellTiter-Glo assays. Statin-responsive genes (HMGCR, LDLR, SREBP-2) are analyzed by qRT-PCR. Each experiment includes other statins as positive controls.
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| Animal Protocol |
In vivo efficacy is evaluated in rodent models of hypercholesterolemia, such as high-fat diet-fed hamsters or LDL receptor knockout mice. PPD 10558 is administered orally at doses ranging from 0.1-100 mg/kg/day. Blood samples are collected for lipid profile analysis (total cholesterol, LDL-C, HDL-C, triglycerides). Liver tissue is collected for cholesterol content measurement and gene expression analysis. For developmental toxicity assessment, pregnant rats and rabbits are administered daily oral doses during organogenesis. Fetal development is evaluated by skeletal and visceral examination. Sample sizes typically range from 6-15 animals per group.
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| ADME/Pharmacokinetics |
PPD 10558 is orally active. Storage: powder at -20°C for 3 years; 4°C for 2 years. In solvent: -80°C for 6 months; -20°C for 1 month. The compound has a molecular weight of 588.67 g/mol. As a statin, it undergoes extensive first-pass hepatic metabolism. Its bioavailability is influenced by hepatic extraction efficiency, which the compound enhances. The compound is lipophilic, typical of statins.
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| Toxicity/Toxicokinetics |
In developmental toxicity studies, daily oral administration to pregnant rats and rabbits during organogenesis showed little toxic effect on development, with a NOAEL of ≥320 mg/kg. As a statin, potential adverse effects include hepatotoxicity, myopathy, and increased risk of diabetes at high doses. Standard toxicology profiling would include acute, subchronic, and chronic toxicity studies, genotoxicity assessment, and carcinogenicity studies. The compound is intended for research use only and has not received regulatory approval.
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| References | |
| Additional Infomation |
PPD 10558 is also known as Bemfivastatin and RBx-10558. It is a statin-class HMG-CoA reductase inhibitor investigated for primary hypercholesterolemia treatment. The compound enhances hepatic extraction activity. It shows a favorable developmental toxicity profile in animal studies. No clinical trials or regulatory approvals have been reported for this compound. It is intended for laboratory research purposes only.
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| Molecular Formula |
C34H37FN2O6
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|---|---|
| Molecular Weight |
588.665793180466
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| Exact Mass |
588.263
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| CAS # |
805241-79-6
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| Related CAS # |
Bemfivastatin hemicalcium;805241-64-9
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| PubChem CID |
23652120
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| Appearance |
White to off-white solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
43
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| Complexity |
869
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PMFRPLBQEYHUMG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H37FN2O6/c1-21(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/h3-15,21,27-28,38-40H,16-20H2,1-2H3,(H,36,43)(H,41,42)
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| Chemical Name |
7-[2-(4-fluorophenyl)-4-[[4-(hydroxymethyl)phenyl]carbamoyl]-3-phenyl-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid
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| Synonyms |
PPD10558; RBx-10558; PPD-10558
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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) |
DMSO : ~100 mg/mL (~169.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6987 mL | 8.4937 mL | 16.9874 mL | |
| 5 mM | 0.3397 mL | 1.6987 mL | 3.3975 mL | |
| 10 mM | 0.1699 mL | 0.8494 mL | 1.6987 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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