AR antagonist 5
AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure[1.
For research use only. We do not sell to patients.
- CAS No.: 2902679-53-0
- Formula: C23H21F3N6O2
- Molecular Weight:470.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
>25 μg/mL
Compound: 30a
|
Dark toxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability incubated for 1 hr by neutral red dye based assay
Dark toxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability incubated for 1 hr by neutral red dye based assay
|
[PMID: 38128906] |
| NIH3T3 | IC50 |
>25 μg/mL
Compound: 30a
|
Phototoxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability preincubated for 1 hr followed by 5 J/cm2 irradiation and subsequent replacement of medium without compound and measured after 24 hrs by neutral red dye based assay
Phototoxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability preincubated for 1 hr followed by 5 J/cm2 irradiation and subsequent replacement of medium without compound and measured after 24 hrs by neutral red dye based assay
|
[PMID: 38128906] |
Chemical Information
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CAS No. 2902679-53-0
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Molecular Weight 470.45
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Formula C23H21F3N6O2
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SMILES
C[C@](CN1CC2CC(N2C3=CC=C(C=C3)C#N)C1)(C(NC4=CN=C(C(C(F)(F)F)=C4)C#N)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
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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.
Purity & Documentation
References
[1]. Wenqiang Zhang, et al. Discovery of (2 S)- N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment. J Med Chem. 2024, 67,1. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)