| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Pitavastatin lactone targets the same enzyme as its parent drug. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis. The lactone metabolite is less active than the parent drug but is a major circulating metabolite in humans.
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|---|---|
| ln Vitro |
In vitro, Pitavastatin lactone is characterized as a major metabolite of Pitavastatin. It is formed when the hydroxy acid form of Pitavastatin undergoes lactonization. The compound is less active as an HMG-CoA reductase inhibitor compared to the parent drug but is an important metabolite for pharmacokinetic studies.
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| ln Vivo |
In vivo, Pitavastatin lactone is a major circulating metabolite following Pitavastatin administration. It is formed in the liver and may contribute to the overall pharmacokinetic profile of the parent drug. The compound is used as a reference standard for analytical method development and quality control applications.
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| Enzyme Assay |
In vitro assays for Pitavastatin lactone typically involve analytical method development using HPLC or LC-MS. The compound is used as a reference standard to identify and quantify the metabolite in Pitavastatin samples. Its retention time and mass spectrum are characterized for method validation.
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| Cell Assay |
For in vitro cell-based assays, Pitavastatin lactone is not typically used, as it is a metabolite and not a pharmacological agent. It could be used to study its potential effects on HMG-CoA reductase activity if necessary, but its primary role is as an analytical reference standard. Cell viability and other cellular effects are not typically assessed for this compound.
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| Animal Protocol |
In vivo animal studies with Pitavastatin lactone are not typically performed, as it is a metabolite and not a therapeutic candidate. Its use is confined to analytical and pharmacokinetic studies. The compound is used as a reference standard for the quantification of Pitavastatin and its metabolites in biological samples.
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| ADME/Pharmacokinetics |
Pitavastatin lactone (CAS: 141750-63-2) has a molecular weight of 403.45 g/mol and a molecular formula of C25H22FNO3. IUPAC name: (4R,6S)-6-((E)-2-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)vinyl)-4-hydroxytetrahydro-2H-pyran-2-one. Appearance: solid powder. Purity: ≥95%. Storage: -20°C.
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| Toxicity/Toxicokinetics |
Pitavastatin lactone is a research compound and is not approved for human therapeutic use. As a metabolite standard, it is used in very small quantities and does not pose significant toxicity risks under normal handling. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Pitavastatin lactone is a major phase 2 metabolite of Pitavastatin, an inhibitor of HMG-CoA reductase. It is formed when the hydroxy acid form of Pitavastatin undergoes lactonization. It has a molecular weight of 403.45 g/mol and a molecular formula of C25H22FNO3. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C25H22FNO3
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|---|---|
| Molecular Weight |
403.44500
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| Exact Mass |
403.158
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| CAS # |
141750-63-2
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| PubChem CID |
9801294
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
616.9±55.0 °C at 760 mmHg
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| Melting Point |
92-95ºC
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| Flash Point |
326.9±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.721
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| LogP |
3.44
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
642
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CC1C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H]4C[C@H](CC(=O)O4)O)C5=CC=C(C=C5)F
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| InChi Key |
XJVKVAFYQRWVAJ-MCBHFWOFSA-N
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| InChi Code |
InChI=1S/C25H22FNO3/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-19-13-18(28)14-23(29)30-19/h1-4,7-12,16,18-19,28H,5-6,13-14H2/b12-11+/t18-,19-/m1/s1
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| Chemical Name |
(4R,6S)-6-[(E)-2-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]ethenyl]-4-hydroxyoxan-2-one
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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) |
DMSO : ~100 mg/mL (~247.86 mM)
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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 | 2.4786 mL | 12.3931 mL | 24.7862 mL | |
| 5 mM | 0.4957 mL | 2.4786 mL | 4.9572 mL | |
| 10 mM | 0.2479 mL | 1.2393 mL | 2.4786 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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