Physicochemical Properties
| Molecular Formula | C28H35CLO12 |
| Molecular Weight | 599.02 |
| Appearance | Typically exists as solid at room temperature |
| 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) |
Biological Activity
| ln Vitro | In bone marrow monocytes/macrophages (BMM with 100% inhibition), pradelolide (compound 21) (10 µM) has anti-osteoclastogenic action [1]. Actin ring formation and osteoclast bone resorption in BMMs are inhibited by pralidoxime (1, 1.25, 5, 10 µM; 1–5 days) without causing cytotoxicity [1]. Praelolide(5, 10 µM) suppresses the mRNA levels of NFATc1, cathepsin K, MMP-9, and TRAP in BMMs that are stimulated by RANKL [1]. The protein expression of Nrf2, HO-1, and NQO1 is increased, and the stability of Nrf2 protein is improved by prallelolide (5, 10 µM; 6 h) [1]. Pre-osteoclasts treated with pralidoxime (10 µM; 0–60 min) exhibit inhibition of RANKL-induced NF-κB and MAPK signaling pathways as well as phosphorylation of ERK, p38 MAPK, IKBα, and p65 NF-κB [1]. By binding to the Keap1 protein in RAW264.7 cells, pralidoxide (0, 20, 50, and 100 µM; 24 h) disrupts the interaction between Keap1 and Nrf2 [1]. |
| ln Vivo | Prednisone-induced bone loss in zebrafish is prevented by protelolide (2, 5, 10 µM; co-treated for 6 days) [1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: Bone marrow monocytes/macrophages(BMMs) Tested Concentrations: 1, 2.5, 5, 10, 20, 30, 40, 50 µM Incubation Duration: 1-5 days Experimental Results: Suppressed RANKL-induced TRAP positive Osteoclasts formation in a time dependent manner, shows no effect on cell viability. RT-PCR[1] Cell Types: Bone marrow monocytes/macrophages(BMMs) Tested Concentrations: 5, 10 µM Incubation Duration: 1-5 days Experimental Results: Inhibited RANKL- induced mRNA levels of NFATc1, cathepsin K, MMP-9 and TRAP. Western Blot Analysis[1] Cell Types: Bone marrow monocytes/macrophages(BMMs), RAW264.7 cells Tested Concentrations: 5, 10 µM Incubation Duration: 6 h Experimental Results: Promoted the protein expression of Nrf2 in the nucleus and HO-1 and NQO1 in the cytoplasm, increased the Nrf2 stability by reducing ubiquitin degradation of Nrf2. |
| Animal Protocol |
Animal/Disease Models: Zebrafish larvae at the age of 3 dpf (day-post-fertilization)[1] Doses: 2, 5, 10 µM Route of Administration: Co-treated for 6 days Experimental Results: Remarkably increased the amount of bone mineralization in prednisolone-treated zebrafish larvae especially at the concentration of 5 μM which even excelled 10 μM praelolide-treated group. |
| References | [1]. Qi X, et al. Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway. Eur J Med Chem. 2022 Nov 24;246:114948. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6694 mL | 8.3470 mL | 16.6939 mL | |
| 5 mM | 0.3339 mL | 1.6694 mL | 3.3388 mL | |
| 10 mM | 0.1669 mL | 0.8347 mL | 1.6694 mL |