AR antagonist 18
AR antagonist 18 is a selective androgen receptor antagonist with an IC50 of 20.6 nM. AR antagonist 18 exerts AR transcriptional inhibitory effects by interacting with AR residues Phe765 and Trp742 via conformational flexibility. AR antagonist 18 acts as a hair growth inducer, and exhibits low systemic exposure and reduced distribution to male reproductive organs in a mouse model of hair growth. AR antagonist 18 can be used for research on androgenetic alopecia.
For research use only. We do not sell to patients.
- CAS No.: 3084436-73-4
- Formula: C19H19N5OS2
- Molecular Weight:397.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
AR antagonist 18 (compound 39) potently inhibits the transcriptional activity of AR in LNCaP cells, with an IC50 of 21 nM; it shows no activity against ERα and ERβ in HEK293T cells, and exhibits over 26-fold higher selectivity for AR over PR, with a PR IC50 of 560 nM[1].
AR antagonist 18 exhibits a high skin tissue binding rate (96.51% at 6 h) and maintains long-lasting stability in C57BL/6 mouse skin homogenates; it is metabolized into inactive or weakly active derivatives in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t |
|---|---|---|---|---|---|---|
| Mice[1] | 600 ug | o.a. | 1.63 h | 0.50 h | 349 ng/mL | 357 ng·h/mL |
AR antagonist 18 (1-2.5%; topical administration; once daily; for 28 consecutive days) shows no obvious systemic toxicity in CD-1 mice, with high skin retention and low systemic exposure in reproductive tissues[1].
AR antagonist 18 (0.6 mg per mouse; topical administration; single dose) exhibits characteristics of high skin retention, low systemic plasma exposure, and lower accumulation in androgen-responsive reproductive tissues compared with pyrilutamide in male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6 weeks old, acclimatized for 1 week, androgenetic alopecia model with shaved dorsal skin, telogen-phase hair follicles)[1]
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Dosage:0.5%
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Administration:topical; twice daily; 37 days
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Result:Exhibited hair growth efficacy equivalent to 0.5% pyrilutamide with faster therapeutic onset (14 days versus 21 days).
Lowered systemic plasma exposure after 37-day continuous dosing, sustained high skin drug levels 24 h post last administration.
Displayed negligible non-accumulative distribution in male reproductive organs, and induced normal body weight fluctuations during treatment.
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Animal Model:CD-1 (6-9 weeks old, 25-35 g, half male and half female, healthy)[1]
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Dosage:1%; 2.5%
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Administration:topical; once daily; 28 days
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Result:Observed no deaths, clinical abnormalities or statistical changes in weight, food consumption, blood biochemistry and organ indexes versus vehicle control.
Detected no drug-related pathological lesions in vital organs and androgen-sensitive reproductive tissues by histopathology.
Delivered high skin drug exposure and low reproductive tissue levels after 28-day 2.5% topical dosing, with reproductive tissue concentrations inferior to 2.5% pyrilutamide.
Chemical Information
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CAS No. 3084436-73-4
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Molecular Weight 397.52
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Formula C19H19N5OS2
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SMILES
CSC1=CC(N2C(N(CC3=CC=C(C)N=C3)C(C)(C)C2=O)=S)=CN=C1C#N
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AR antagonist 18 Related Classifications
HY-187369 Related Classifications
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