| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
p65
Rubiadin-1-methyl ether inhibits osteoclastic bone resorption by inhibiting the phosphorylation level of NF-kappaB p65, degrading IkappaBalpha protein, and reducing the nuclear translocation of p65. It also enhances adipocyte differentiation in 3T3-L1 cells. |
|---|---|
| ln Vitro |
In vitro, Rubiadin-1-methyl ether enhances adipocyte differentiation in 3T3-L1 cells. It can be used as a drug to treat osteosarcoma. It inhibits osteoclast formation and bone resorption.
|
| ln Vivo |
In vivo, Rubiadin-1-methyl ether has been shown to inhibit osteoclast activity and bone resorption in animal models of bone loss. It has potential for the treatment of osteoporosis and osteosarcoma.
|
| Enzyme Assay |
A non-cell assay for NF-kappaB inhibition uses a luciferase reporter gene system. Rubiadin-1-methyl ether is added to the reaction, and luciferase activity is measured. Alternatively, EMSA is used to assess inhibition of NF-kappaB DNA binding activity.
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| Cell Assay |
For cell studies, Rubiadin-1-methyl ether is dissolved in DMSO and diluted in culture medium. RAW 264.7 macrophages are treated with RANKL to induce osteoclast differentiation in the presence or absence of the compound. TRAP staining is used to quantify osteoclast formation.
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| Animal Protocol |
In animal studies, Rubiadin-1-methyl ether is typically administered to rodents by oral gavage or intraperitoneal injection. It is used in models of osteoporosis (e.g., ovariectomized mice) and osteosarcoma. Bone mineral density and histology are assessed.
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| ADME/Pharmacokinetics |
Limited PK data are available. The compound is likely absorbed from the gut and distributed to bone tissue. It may undergo phase II metabolism (glucuronidation).
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| Toxicity/Toxicokinetics |
The compound is generally considered safe at research doses. No significant toxicity has been reported in animal studies. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
Rubiadin 1-methyl ether has been reported in Hymenodictyon orixense, Coelospermum paniculatum, and other organisms with available data.
Rubiadin-1-methyl ether is a natural product used as a research tool for studying osteoclast biology and bone resorption. It has potential therapeutic applications for osteoporosis, osteosarcoma, and other bone disorders. It is not an approved drug. |
| Molecular Formula |
C16H12O4
|
|---|---|
| Molecular Weight |
268.26
|
| Exact Mass |
268.073
|
| CAS # |
7460-43-7
|
| PubChem CID |
96191
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
502.2±50.0 °C at 760 mmHg
|
| Flash Point |
193.0±23.6 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.649
|
| LogP |
3.92
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
419
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C=C2C(=C1OC)C(=O)C3=CC=CC=C3C2=O)O
|
| InChi Key |
NTBUBTCXACOEEC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12O4/c1-8-12(17)7-11-13(16(8)20-2)15(19)10-6-4-3-5-9(10)14(11)18/h3-7,17H,1-2H3
|
| Chemical Name |
3-hydroxy-1-methoxy-2-methylanthracene-9,10-dione
|
| 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) |
DMSO :≥ 125 mg/mL (~465.97 mM)
|
|---|---|
| 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 | 3.7277 mL | 18.6386 mL | 37.2773 mL | |
| 5 mM | 0.7455 mL | 3.7277 mL | 7.4555 mL | |
| 10 mM | 0.3728 mL | 1.8639 mL | 3.7277 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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