| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Calcium channels (calcium antagonist); targets involved in polymorphonuclear leukocyte (PMN) influx and IL-6 release.
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|---|---|
| ln Vitro |
In vitro, Praeruptorin E relaxes swine coronary artery and decreases contractility in guinea-pig left atria, effects similar to calcium entry blocking drugs. It also inhibits polymorphonuclear leukocyte influx, IL-6 release, and protein exudation in cellular models of lung injury. pD2' value: 5.2 (calcium antagonism).
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| ln Vivo |
In vivo, Praeruptorin D and E protect mice from hydrochloric acid (HCl)-induced lung injury by inhibiting PMN influx, IL-6 release, and protein exudation. These findings suggest they may be useful in the therapy of lung injury. Detailed dose-response and pharmacokinetic data in vivo are limited.
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| Enzyme Assay |
No specific cell-free enzyme/receptor binding assay protocol is detailed for Praeruptorin E. As a calcium channel antagonist, typical cell-free assays involve radioligand binding to purified L-type calcium channels or measuring calcium flux using fluorescent indicators in membrane preparations. IC50 or Ki values are calculated from competition binding curves.
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| Cell Assay |
Calcium channel blocking activity is assessed in isolated tissue preparations (swine coronary artery, guinea-pig left atria). Tissues are mounted in organ baths, contracted with depolarizing agents (e.g., high K+), and relaxation responses to Praeruptorin E are measured. pD2' values are calculated from concentration-response curves. Anti-inflammatory effects are evaluated in PMN migration assays and IL-6 release assays in cultured cells.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of HCl-induced lung injury. Praeruptorin E is administered (route not specified in available literature) before or after HCl challenge. Endpoints include bronchoalveolar lavage fluid analysis (PMN count, IL-6 levels, protein exudation) and histopathological examination of lung tissue.
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| ADME/Pharmacokinetics |
Molecular weight: 428.47; molecular formula: C24H28O7. Purity: ≥98%. Storage: 2-8°C, tightly sealed, stable for up to 24 months. Solubility: ethanol (soluble), DMSO (4.29 mg/mL), pyridine, methanol (soluble). Density: 1.22 g/cm³.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural pyranocoumarin from a traditional medicinal plant, it is generally considered to have low toxicity, but standard toxicological profiling would be required for drug development.
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| References | |
| Additional Infomation |
Reports indicate that Praeruptorin E has been found in Musineon divaricatum, and relevant data is available for reference.
Praeruptorin E is a research-grade compound, not approved for therapeutic use. It is primarily used as a pharmacological tool for studying calcium channel biology and lung protection. No clinical trials or FDA approval have been reported. Its mechanism involves calcium channel antagonism and inhibition of inflammatory responses in lung injury. |
| Molecular Formula |
C24H28O7
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|---|---|
| Molecular Weight |
428.4749
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| Exact Mass |
428.183
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| CAS # |
78478-28-1
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| PubChem CID |
6440581
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
516.5±50.0 °C at 760 mmHg
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| Flash Point |
221.4±30.2 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.560
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| LogP |
5.59
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
779
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C/C=C(/C)\C(=O)O[C@H]1[C@H](C2=C(C=CC3=C2OC(=O)C=C3)OC1(C)C)OC(=O)CC(C)C
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| InChi Key |
UFUVJROSOIXJGR-WLISBCLRSA-N
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| InChi Code |
InChI=1S/C24H28O7/c1-7-14(4)23(27)30-22-21(29-18(26)12-13(2)3)19-16(31-24(22,5)6)10-8-15-9-11-17(25)28-20(15)19/h7-11,13,21-22H,12H2,1-6H3/b14-7-/t21-,22-/m0/s1
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| Chemical Name |
[(9S,10S)-8,8-dimethyl-10-(3-methylbutanoyloxy)-2-oxo-9,10-dihydropyrano[2,3-f]chromen-9-yl] (Z)-2-methylbut-2-enoate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~25 mg/mL (~58.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3339 mL | 11.6694 mL | 23.3389 mL | |
| 5 mM | 0.4668 mL | 2.3339 mL | 4.6678 mL | |
| 10 mM | 0.2334 mL | 1.1669 mL | 2.3339 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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