| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
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| Other Sizes |
| Targets |
4.84 μM (A-549 cells) and 7.06 μM (HepG2 cells)[1]
Periplocoside M targets cancer cells, exhibiting cytotoxic activity against human A-549 and HepG2 cell lines. The compound's mechanism of action is not well characterized but may involve disruption of cellular processes essential for cancer cell survival. As a cardiac glycoside-like compound, it may inhibit the Na+/K+-ATPase pump, leading to changes in intracellular ion concentrations and induction of apoptosis. However, specific molecular targets have not been identified. |
|---|---|
| ln Vitro |
In vitro, periplocoside M exhibits inhibitory effects on human A-549 lung cancer cells and HepG2 liver cancer cells, with IC50 values of 4.84 μM and 7.06 μM, respectively. These data indicate that periplocoside M has potent antiproliferative activity against these cancer cell lines. The compound's activity suggests potential for further development as an anticancer agent. However, detailed mechanism of action studies are limited.
|
| ln Vivo |
In vivo activity of periplocoside M has not been extensively reported. As a compound with in vitro antitumor activity, it may have potential for treating cancer in vivo. However, no specific in vivo efficacy data are available from publicly accessible sources. The compound is not used as a therapeutic agent and has no approved clinical indications.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for periplocoside M would typically involve screening against a panel of targets to identify its mechanism of action. Given its structural similarity to cardiac glycosides, assays for Na+/K+-ATPase inhibition would be relevant. The compound is incubated with the enzyme in the presence of ATP and ions, and enzyme activity is measured by monitoring phosphate release or using coupled enzyme assays. Binding to other targets such as topoisomerases or kinases could also be assessed.
|
| Cell Assay |
In vitro cell-based assays for periplocoside M involve culturing cancer cell lines (A-549 and HepG2) and treating them with the compound to assess effects on cell proliferation. Cells are seeded in multi-well plates, treated with various concentrations of periplocoside M for 24-72 hours, and cell viability is assessed using MTT, CellTiter-Glo, or SRB assays. IC50 values are calculated from dose-response curves. Apoptosis and cell cycle analysis can be performed using flow cytometry.
|
| Animal Protocol |
In vivo animal studies for periplocoside M have not been reported in the literature. If conducted, such studies might involve mouse xenograft models of lung or liver cancer, where the compound is administered orally or intraperitoneally and tumor growth is monitored. Standard protocols for xenograft studies would be employed. No specific data are available.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of periplocoside M have not been characterized. As a glycoside with a molecular weight of 604.77, it is expected to have limited oral bioavailability due to poor absorption and extensive first-pass metabolism. Glycosides are typically hydrolyzed by gut microbiota or intestinal enzymes to release the aglycone, which may then be absorbed. No specific PK data are available.
|
| Toxicity/Toxicokinetics |
The toxicity profile of periplocoside M has not been systematically evaluated. As a cardiac glycoside-like compound, it may have cardiotoxicity at high doses, similar to other compounds in this class. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology, with special attention to cardiac effects. No specific toxicity data are available.
|
| References | |
| Additional Infomation |
Reports indicate that Periploca sepium contains (2R,6R)-6-[[(3S,8R,9S,10R,13S,14S,17R)-17-[(1S)-1-[(2S,4R,5S,6R)-4,5-dihydroxy-6-methyloxacyclohexane-2-yl]oxyethyl]-17-hydroxy-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecylhydrocyclopenta[a]phenanthrene-3-yl]oxy]-4-methoxy-2-methyl-2H-pyran-5-one, and related data have been reported.
Periplocoside M is a C21 pregnane glycoside isolated from Periploca sepium root bark. It has the molecular formula C34H52O9 and a molecular weight of 604.77. The compound exhibits antitumor activity against A-549 and HepG2 cancer cell lines with IC50 values of 4.84 and 7.06 μM, respectively. Periplocoside M is a research compound with potential applications in cancer research. It is not approved for clinical use. |
| Molecular Formula |
C34H52O9
|
|---|---|
| Molecular Weight |
604.77
|
| Exact Mass |
604.361
|
| CAS # |
116782-73-1
|
| PubChem CID |
131845091
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
735.6±60.0 °C at 760 mmHg
|
| Flash Point |
227.8±26.4 °C
|
| Vapour Pressure |
0.0±5.5 mmHg at 25°C
|
| Index of Refraction |
1.575
|
| LogP |
4.63
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
43
|
| Complexity |
1140
|
| Defined Atom Stereocenter Count |
14
|
| SMILES |
O[C@]1([C@H](C)O[C@@H]2C[C@@H]([C@@H]([C@H](C)O2)O)O)CC[C@H]2[C@@H]3CC=C4C[C@H](CC[C@]4(C)[C@H]3CC[C@@]21C)O[C@H]1C(C(=C[C@H](C)O1)OC)=O
|
| InChi Key |
CGUNKFNCRCGQRL-OIFJRFLVSA-N
|
| InChi Code |
InChI=1S/C34H52O9/c1-18-15-27(39-6)30(37)31(40-18)43-22-9-12-32(4)21(16-22)7-8-23-24(32)10-13-33(5)25(23)11-14-34(33,38)20(3)42-28-17-26(35)29(36)19(2)41-28/h7,15,18-20,22-26,28-29,31,35-36,38H,8-14,16-17H2,1-6H3/t18-,19-,20+,22+,23-,24+,25+,26-,28+,29-,31+,32+,33+,34+/m1/s1
|
| Chemical Name |
(2R,6R)-6-[[(3S,8R,9S,10R,13S,14S,17R)-17-[(1S)-1-[(2S,4R,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxyethyl]-17-hydroxy-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-yl]oxy]-4-methoxy-2-methyl-2H-pyran-5-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.6535 mL | 8.2676 mL | 16.5352 mL | |
| 5 mM | 0.3307 mL | 1.6535 mL | 3.3070 mL | |
| 10 mM | 0.1654 mL | 0.8268 mL | 1.6535 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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