Tan-931
Tan-931 is a non-competitive and selective inhibitor of aromatase , with an IC50 is 17.2 μM and a Ki of 40 μM for human aromatase, and an IC50 of 162 μM for rat aromatase. Tan-931 reduces plasma estradiol-17β level and weight of ovaries and uterus in PMSG (HY-N12634)-treated female rats. Tan-931 can be used for the research of estrogen-dependent metastatic breast cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 127448-92-4
- Formule: C15H10O7
- Masse moléculaire:302.24
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
|
Aromatase 17.2 μM (IC50) |
Aromatase 40 μM (Ki) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MDCK | IC50 |
58.6 μM
Compound: 7, TAN-931
|
Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as compound concentration required for inhibiting influenza virus yield at 48 h post-infection by crystal violet staining based CPE inhibition assay
Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as compound concentration required for inhibiting influenza virus yield at 48 h post-infection by crystal violet staining based CPE inhibition assay
|
[PMID: 21879714] |
In Vitro
Tan-931 weakly inhibits aromatase in a microsomal assay with an IC50 of 17.2 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Tan-931 (100 mg/kg; s.c., twice daily for 7 days) dose not induce adrenal hypertrophy in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female Sprague-Dawley (20-day-old) challenged with PMSG[1]
-
Dosage:25, 50, 100 mg/kg
-
Administration:s.c.; daily for 4 days
-
Result:Reduced PMSG-induced increases in plasma estradiol-17β level and ovarian weight in a dose-dependent manner.
Reduced plasma estradiol-17β.
Slightly reduced uterine weight.
Reduced total and specific ovarian aromatase activity.
-
Animal Model:Sprague-Dawley (9-week-old male)[1]
-
Dosage:100 mg/kg
-
Administration:s.c., twice daily for 7 days
-
Result:Did not induce adrenal hypertrophy.
Caused a significant increase in body weight.
Did not affect liver weight relative to controls.
Chemical Information
-
CAS No. 127448-92-4
-
Masse moléculaire 302.24
-
Formule C15H10O7
-
SMILES
O=CC1=CC(C(O)=O)=CC(O)=C1C(C2=C(O)C=CC=C2O)=O
-
Structure Classification
-
Initial Source
Penicillium funiculosum
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
-
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
Références
[1]. Ishii T, et al. TAN-931, a novel nonsteroidal aromatase inhibitor produced by Penicillium funiculosum No. 8974. I. Taxonomy, fermentation, isolation,characterization and biological activities. J Antibiot (Tokyo). 1991 Jun;44(6):589-99. [Content Brief]
[2]. Balunas MJ, et al. Natural products as aromatase inhibitors. Anticancer Agents Med Chem. 2008 Aug;8(6):646-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tan-931 Related Classifications
HY-180420 Related Classifications
Powered by Bioz