Cyproterone acetate

SKU: orb1225070

Description

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.(In Vitro):Cyproterone acetate is a partial agonist, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations.Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5.Cyproterone acetate pretreatment (0,1,10, or 50 μM; 24 hours; subsequently exposed to cadmium for an additional 24 hours) resulted in a clear decrease in the sensitivity to cadmium in rat liver epithelial cell line.(In Vivo):Adult male C57 BL/6J mice injected with 0.08 mg/g of cyproterone acetate showed an increase in cellular lipid content in the zona fasciculata and zona retjculans of the adrenal cortex.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	427-51-0
MW	416.94
Purity	>98% (HPLC)
Formula	C₂₄H₂₉ClO₄
SMILES	CC(O[C@]1(C(C)=O)CC[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)[C@](C5)([H])[C@]5([H])C(C=C4C(Cl)=C[C@@]23[H])=O)=O
Target	Androgen Receptor (AR)
Solubility	Ethanol: 10 mg/mL (23.98 mM); DMSO: 83 mg/mL (199.06 mM)

Bioactivity

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In Vivo

Adult male C57 BL/6J mice injected with 0.08 mg/g of cyproterone acetate showed an increase in cellular lipid content in the zona fasciculata and zona retjculans of the adrenal cortex.

In Vitro

Cyproterone acetate is a partial agonist, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5.Cyproterone acetate pretreatment (0, 1, 10, or 50 μM; 24 hours; subsequently exposed to cadmium for an additional 24 hours) resulted in a clear decrease in the sensitivity to cadmium in rat liver epithelial cell line.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Androcur | CPA | Cyprostat | NSC 81430 | SH 714

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Quick Database Links

Gene Symbol

Androgen Receptor (AR)

Protocol Information

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Purity:	99.41% (May vary between batches)
CAS Number:	13311-84-7
MW:	276.21
Formula:	C₁₁H₁₁F₃N₂O₃

Purity:	98.43% (May vary between batches)
CAS Number:	427-51-0
MW:	416.94
Formula:	C₂₄H₂₉ClO₄