| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Physalin A targets multiple cellular pathways, including NF-κB, STAT3, and MAPK. It is an anti-inflammatory compound that blocks the activation of the NF-kappaB signaling pathway. It regulates the Nrf2 pathway through ERK and p38 to induce detoxification enzymes. Physalin A reduces mammosphere formation by reducing the expression of the GLI1 gene and the YAP1 gene. It induces apoptosis associated with upregulation of caspase-3 and caspase-8 expression.
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|---|---|
| ln Vitro |
In vitro, Physalin A inhibits the growth of various human tumor cell lines. HT1080 and A375-S2 cells are the most sensitive tumor cell lines. It inhibits HT1080 cell growth in a time- and dose-dependent manner with an IC₅₀ value (at 24 h) of 10.7 μM. It induces apoptosis and is associated with upregulation of caspase-3 and caspase-8 expression. Physalin A induces autophagy and antagonizes the apoptosis of HT1080 cells. It has the potential for the research of cancer disease.
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| ln Vivo |
In vivo, Physalin A has antitumor effect in H292 xenograft tumor model at 40-80 mg/kg via intraperitoneal injection for 10 days. In a mouse osteoarthritis model, intra-articular injection of Physalin A (1 mg/kg) decreased MMP13 production and increased collagen II and aggrecan production. The OARSI score indicated that injecting Physalin A into the joint had a protective effect.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Physalin A involves measuring its effects on various signaling pathways. The compound's ability to block NF-κB activation and regulate Nrf2 pathway through ERK and p38 is assessed. Its binding affinity to target proteins is measured using pull-down assays or surface plasmon resonance. The compound's effects on caspase-3 and caspase-8 expression are evaluated as markers of apoptosis.
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| Cell Assay |
In vitro cell-based assays for Physalin A involve treating various human tumor cell lines (HT1080 fibrosarcoma, A375-S2 melanoma, HepG2 hepatoma, HeLa cervical carcinoma, A549 alveolar basal epithelial, U937 histocytic lymphoma, HCT116 colon cancer, A431 epidermoid carcinoma, MCF7 breast cancer, and HL60 promyelocytic leukemia cells) with 0-80 μM Physalin A for 24 h. Cell viability and proliferation are assessed. Apoptosis is measured by caspase-3 and caspase-8 activation.
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| Animal Protocol |
In vivo animal studies for Physalin A involve xenograft tumor models (H292) where mice are treated with 40-80 mg/kg Physalin A via intraperitoneal injection for 10 days. In a mouse osteoarthritis model, Physalin A is administered via intra-articular injection at 1 mg/kg twice per week. Tumor growth inhibition, MMP13 production, collagen II, and aggrecan production are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Physalin A are not detailed in the available literature. The compound is a natural product with complex structure. For storage, powder should be kept at -20°C.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Physalin A are available in the provided literature. The compound is for research use only and not for human therapeutic applications. Standard laboratory safety precautions should be followed when handling.
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| References | |
| Additional Infomation |
Rasfonin A is a type of Rasfonin. (1S,2S,3R,5R,6S,7R,14R,15S,18R,21S,22R)-5,7,18-trihydroxy-1,14,21-trimethyl-25-methylene-4,20,23-trioxaheptacyclo[20.3.1.12,5.03,18.03,21.06,15.09,14]heptacyclo-8,11-diene-13,19,24,27-tetraone has been reported in Solanaceae plants, Rasfonin lagascae, and other organisms with available data.
Physalin A is a bioactive withanolide with prominent anti-cancer properties. It exhibits significant antitumor activity by inducing apoptosis, enhancing reactive oxygen species (ROS) production, and causing G₂/M phase cell cycle arrest. It is isolated from P. alkekengi. It is a valuable lead compound for drug discovery. Its CAS number is 23027-91-0. |
| Molecular Formula |
C28H30O10
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|---|---|
| Molecular Weight |
526.5318
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| Exact Mass |
526.184
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| CAS # |
23027-91-0
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| PubChem CID |
44577487
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| Appearance |
White to off-white solid powder
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| LogP |
0.429
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
38
|
| Complexity |
1350
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| Defined Atom Stereocenter Count |
11
|
| SMILES |
C[C@]12C[C@H]([C@]3([C@]45[C@H]1C(=O)[C@](O4)([C@H]6[C@H](CC[C@@]5(C(=O)O3)O)[C@@]7(C(=C[C@H]6O)CC=CC7=O)C)O)C)OC(=O)C2=C
|
| InChi Key |
VELDODQHYQSJOF-RPKVKFPNSA-N
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| InChi Code |
InChI=1S/C28H30O10/c1-12-21(32)36-17-11-23(12,2)19-20(31)27(35)18-14(24(3)13(10-15(18)29)6-5-7-16(24)30)8-9-26(34)22(33)37-25(17,4)28(19,26)38-27/h5,7,10,14-15,17-19,29,34-35H,1,6,8-9,11H2,2-4H3/t14-,15+,17+,18-,19-,23+,24-,25-,26-,27+,28-/m0/s1
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| Chemical Name |
(1S,2S,3R,5R,6S,7R,14R,15S,18R,21S,22R)-5,7,18-trihydroxy-1,14,21-trimethyl-25-methylidene-4,20,23-trioxaheptacyclo[20.3.1.12,5.03,18.03,21.06,15.09,14]heptacosa-8,11-diene-13,19,24,27-tetrone
|
| 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) |
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 | 1.8992 mL | 9.4961 mL | 18.9923 mL | |
| 5 mM | 0.3798 mL | 1.8992 mL | 3.7985 mL | |
| 10 mM | 0.1899 mL | 0.9496 mL | 1.8992 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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