| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
VEGF/VEGFR and Ang2/Tie2 signaling pathways. 5alpha-Hydroxycostic acid is a natural product inhibitor of choroidal neovascularization, acting through these dual signaling pathways. It also targets the androgen receptor (AR) to inhibit inflammation.
|
|---|---|
| ln Vitro |
5alpha-Hydroxycostic acid inhibits the viability of rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs) and downregulates pro-inflammatory cytokines. In human breast cancer cells, it exhibits anti-angiogenic and anti-inflammatory effects. It also inhibits choroidal neovascularization (CNV) in a rat model.
|
| ln Vivo |
In a rat model of choroidal neovascularization (CNV), 5alpha-Hydroxycostic acid effectively suppresses the formation of new blood vessels, demonstrating its in vivo anti-angiogenic activity. This dual pathway inhibition (VEGF and Ang2) suggests it could be effective for treating neovascular eye diseases like age-related macular degeneration.
|
| Enzyme Assay |
Cell-free enzyme assays can be performed to assess inhibition of the VEGFR2 kinase. A recombinant VEGFR2 enzyme is incubated with a peptide substrate and ATP. The compound is added, and kinase activity is measured using a luminescent ADP detection kit, allowing for the calculation of an IC50 for the VEGFR2 pathway.
|
| Cell Assay |
Human breast cancer cells or RA-FLSs are seeded in 96-well plates and treated with a range of 5alpha-Hydroxycostic acid concentrations for 24-48 hours. Cell viability is measured by the CCK-8 assay. Inflammatory cytokines in the supernatant are quantified by ELISA. The expression of the androgen receptor (AR) is measured by Western blot.
|
| Animal Protocol |
A laser-induced CNV rat model is used to study anti-angiogenic effects. Male Brown Norway rats receive laser photocoagulation to disrupt Bruch's membrane. 5alpha-Hydroxycostic acid is administered by intravitreal injection. After 14 days, the area of CNV is measured in flat-mounted choroids stained with isolectin B4.
|
| ADME/Pharmacokinetics |
No specific pharmacokinetic data are reported. As a natural product, it is likely to have moderate bioavailability and a short half-life. Its solubility in aqueous buffers is limited, and it is typically formulated in DMSO for in vitro studies. The compound has a molecular weight of 250.33.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are reported. As a natural plant sesquiterpene, it is expected to have a tolerable safety profile. However, formal toxicity studies have not been published. It is a research chemical and is not an approved drug.
|
| References | |
| Additional Infomation |
5β-hydroxymatrine has reportedly been found in Pluchea dioscoridis, Apalochlamys spectabilis, and other organisms with available data.
Other information: 5alpha-Hydroxycostic acid is a bioactive sesquiterpene found in the She medicine Artemisia lavandulaefolia. It has potential for treating rheumatoid arthritis by up-regulating AR expression and for treating neovascular eye diseases by inhibiting VEGF and Ang2 pathways. Purity is typically >96%. CAS number: 132185-83-2. |
| Molecular Formula |
C15H22O3
|
|---|---|
| Molecular Weight |
250.33
|
| Exact Mass |
250.156
|
| CAS # |
132185-83-2
|
| PubChem CID |
637286
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
406.4±38.0 °C at 760 mmHg
|
| Flash Point |
213.8±23.3 °C
|
| Vapour Pressure |
0.0±2.1 mmHg at 25°C
|
| Index of Refraction |
1.540
|
| LogP |
3.19
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
412
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@]12CCCC(=C)[C@]1(C[C@@H](CC2)C(=C)C(=O)O)O
|
| InChi Key |
UEQIFFFWXPAQCB-YUELXQCFSA-N
|
| InChi Code |
InChI=1S/C15H22O3/c1-10-5-4-7-14(3)8-6-12(9-15(10,14)18)11(2)13(16)17/h12,18H,1-2,4-9H2,3H3,(H,16,17)/t12-,14-,15+/m1/s1
|
| Chemical Name |
2-[(2R,4aR,8aS)-8a-hydroxy-4a-methyl-8-methylidene-2,3,4,5,6,7-hexahydro-1H-naphthalen-2-yl]prop-2-enoic acid
|
| 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 | 3.9947 mL | 19.9736 mL | 39.9473 mL | |
| 5 mM | 0.7989 mL | 3.9947 mL | 7.9895 mL | |
| 10 mM | 0.3995 mL | 1.9974 mL | 3.9947 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
