| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Physalin B targets multiple cellular pathways involved in inflammation, proliferation, and apoptosis. It inhibits NF-κB and NLRP3 through activation of the PI3K/Akt pathway. It also activates the Nrf2 pathway to inhibit PDGF-BB-induced vascular smooth muscle cell proliferation and migration. The compound exerts antitumor activity by inhibiting LAP2α-HDAC1-mediated deacetylation of glioma-associated oncogene 1.
|
|---|---|
| ln Vitro |
In cell-free biochemical systems, Physalin B inhibits NF-κB and NLRP3 signaling through activation of the PI3K/Akt pathway. It activates the Nrf2 pathway, leading to antioxidant and anti-inflammatory effects. The compound's ability to modulate these pathways can be assessed using cell-free kinase assays and reporter systems. Physalin B shows potent anti-Trypanosoma cruzi and antimalarial activities.
|
| ln Vivo |
In cell-based assays, Physalin B inhibits the activity of HCT116 cells with an IC50 of 1.35 μmol/L. Treatment with Physalin B (2.5-10 μmol/L) induces apoptosis, PARP and caspase-3 cleavage. The compound also induces autophagosome formation, LC3-II and p62 accumulation, and decreases Beclin 1 protein levels. Physalin B can inhibit the growth of several human leukemia cells and has potential for the treatment of malignant melanoma.
|
| Enzyme Assay |
The cell-free assay for Physalin B involves measuring its effects on purified enzymes and signaling proteins. The compound's inhibition of NF-κB and NLRP3 can be assessed using kinase assays with purified IKK and other components. Its ability to activate Nrf2 can be evaluated using cell-free transcription assays. The compound's binding to target proteins can be studied using surface plasmon resonance or isothermal titration calorimetry.
|
| Cell Assay |
Cell-based assays for Physalin B involve culturing cancer cell lines such as HCT116, breast cancer cells, and leukemia cells. Cells are treated with the compound at concentrations ranging from 0.1 to 100 μmol/L. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V staining, caspase activity assays, and PARP cleavage. Autophagy is assessed by measuring LC3-II and p62 levels. Cell cycle analysis is performed by flow cytometry.
|
| Animal Protocol |
In animal models, Physalin B has been evaluated for its anti-inflammatory and anti-tumor activities. Typical studies involve administration of the compound to mice via intraperitoneal or oral routes. In models of acute lung injury, Physalin B ameliorates lipopolysaccharide-induced inflammatory responses. Tumor-bearing mice are used to assess anti-tumor efficacy. Tissues are collected for analysis of inflammatory markers, apoptosis, and signaling pathway modulation.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Physalin B have not been extensively reported. As a seco-steroidal compound with a molecular weight of 510.54 g/mol, it would be expected to have moderate oral bioavailability and tissue penetration. The compound is typically stored at 4°C, protected from light. It is soluble in DMSO. Further pharmacokinetic studies would be required for therapeutic development.
|
| Toxicity/Toxicokinetics |
Physalin B is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this natural product. As a compound with diverse biological activities, it may have effects on multiple cellular processes. The compound is typically stored at 4°C, protected from light. Standard toxicity studies would be required for therapeutic development.
|
| References |
|
| Additional Infomation |
It has been reported that (1R,2S,5R,8S,9R,17R,18R,21S,24R,26S,27S)-5-hydroxy-2,9,26-trimethyl-3,19,23,28-tetraoxaoctane[16.9.1.118,27.01,5.02,24.08,17.09,14.021,26]nonadecano-11,14-diene-4,10,22,29-tetraone exists in the Solanaceae plants Witheringia solanacea and Physalis lagascae, as well as other organisms with available data.
Physalin B is a research-grade natural product supplied for inflammation and cancer research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a bioactive seco-steroidal compound from Physalis angulata. It has a wide range of biological activities for the treatment of inflammatory conditions and cancer. This product is intended for research use only. |
| Molecular Formula |
C28H30O9
|
|---|---|
| Molecular Weight |
510.53
|
| Exact Mass |
510.189
|
| CAS # |
23133-56-4
|
| PubChem CID |
11613161
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.557
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
37
|
| Complexity |
1300
|
| Defined Atom Stereocenter Count |
11
|
| SMILES |
C[C@]12C[C@@H]3[C@]4([C@]56[C@H]1C(=O)[C@](O5)([C@@H]7CC=C8CC=CC(=O)[C@@]8([C@H]7CC[C@@]6(C(=O)O4)O)C)OC[C@H]2C(=O)O3)C
|
| InChi Key |
HVTFEHJSUSPQBK-DNJDGUCCSA-N
|
| InChi Code |
InChI=1S/C28H30O9/c1-23-11-18-25(3)28-19(23)20(30)27(37-28,34-12-16(23)21(31)35-18)15-8-7-13-5-4-6-17(29)24(13,2)14(15)9-10-26(28,33)22(32)36-25/h4,6-7,14-16,18-19,33H,5,8-12H2,1-3H3/t14-,15+,16-,18+,19-,23+,24-,25-,26-,27+,28-/m0/s1
|
| Chemical Name |
(1R,2S,5R,8S,9R,17R,18R,21S,24R,26S,27S)-5-hydroxy-2,9,26-trimethyl-3,19,23,28-tetraoxaoctacyclo[16.9.1.118,27.01,5.02,24.08,17.09,14.021,26]nonacosa-11,14-diene-4,10,22,29-tetrone
|
| 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 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)
|
| 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 | 1.9587 mL | 9.7937 mL | 19.5875 mL | |
| 5 mM | 0.3917 mL | 1.9587 mL | 3.9175 mL | |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9587 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
