| CAS |
427-51-0 |
| Chinese Name |
醋酸环丙氯地孕酮 |
| English Name |
Cyproterone Acetate |
| Synonyms |
Androcur;Cyproterone 17-O-acetate;醋酸环丙孕酮 |
| Molecular Formula |
C24H29ClO4 |
| Molecular Weight |
416.94 |
| Solubility |
Soluble in DMSO≥10mg/mL；Soluble in Ethanol≥1mg/mL；Soluble in Water＜1mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 207-048-3 |
| MDL |
MFCD00192402 |
| SMILES |
C[C@@]12C(C(Cl)=C[C@]3([H])[C@]2([H])C[C@@]4(C)[C@@]3([H])CC[C@]4(OC(C)=O)C(C)=O)=CC([C@H]5[C@@H]1C5)=O |
| InChIKey |
UWFYSQMTEOIJJG-FDTZYFLXSA-N |
| InChI |
InChI=1S/C24H29ClO4/c1-12(26)24(29-13(2)27)8-6-16-14-10-20(25)19-11-21(28)15-9-18(15)23(19,4)17(14)5-7-22(16,24)3/h10-11,14-18H,5-9H2,1-4H3/t14-,15+,16-,17-,18-,22-,23-,24-/m0/s1 |
| PubChem CID |
9880 |
| Target Point |
Androgen Receptor |
| Passage |
Endocrinology & Hormones |
| Background |
Cyproterone Acetate is an androgen receptor antagonist. |
| Biological Activity |
是雄激素受体拮抗剂，IC50为7.1 nM，也是微弱的孕激素受体激动剂，具有微弱的孕激素和糖皮质激素活性。[1] |
| IC50 |
Androgen Receptor: 7.1nM [1] |
| In Vitro |
Cyproterone acetate具有显著的拮抗性能，也具有部分激活剂特性，在浓度相对较高时激活AR，EC50为4.0 μM。[1] 在10 nM 睾丸激素存在时，低浓度Cyproterone acetate抑制T-刺激的3XHRE-LUC转录，但是高浓度时刺激转录。[2] |
| In Vivo |
Cyproterone acetate作用于生殖器官对重量有直接的负面影响，且显著降低精子数量和 Ca2+含量。 Cyproterone acetate处理的大鼠中，SOD和GST活性显著降低，NO显著提高，MDA含量反应睾丸的氧化状态。[3] |
| Animal Experiment |
Rats were divided into 5 groups treated daily via an oral tube for two intervals 2 and 4 weeks，1st control，2nd E(Echinacea treated group in dose 63 mg kg(-1))，3rd CA(cyproterone acetate treated group in dose 25 mg kg(-1))，4th E+CA and 5th E as prophylactic one week before E+CA treatment with the same aforementioned E or CA doses. The body，testes，epididymis and vas deferens weights were recorded.[3] |
| Data Literature Source |
[1] Sonneveld E，et al. Toxicol Sci. 2005，83(1)，136-148.
[2] Attardi BJ，et al. Mol Cell Endocrinol. 2010，328(1-2)，16-21.
[3] Arafa NM. Pak J Biol Sci. 2010，13(20)，966-976. |
| Unit |
Bottle |
| Specification |
50mg 100mg |
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