| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D656087-1ml |
1ml |
期货  |
|
| 别名 | D4-阿比特龙 |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | D4-abiraterone |
| 生化机理 | D4-阿比特龙是阿比特龙的主要代谢产物。D4-阿比特龙是 CYP17A1、3b-羟基类固醇脱氢酶（3βHSD）和类固醇-5a-还原酶（SRD5A）的抑制剂，也是雄激素受体的拮抗剂。 |
| 储存温度 | 充氩,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1 , 3b-hydroxysteroid dehydrogenase ( 3βHSD ) and steroid-5a-reductase ( SRD5A ) and also an antagonist of androgen receptor . In Vitro D4-abiraterone (D4A ) (10 mM) nearly completely blocks conversion from D4-androstenedione (AD) to 5α-androstanedione and other 5α-reduced androgens. The affinity of D4-abiraterone for mutant (expressed in LNCaP, half-maximum inhibitory concentration (IC 50 =5.3 nM)) and wild type (expressed in LAPC4, IC 50 =7.9 nM) androgen receptor (AR) is greater than that of abiraterone (Abi) (IC 50 =418 and >500 nM, respectively). Compare with Abi, D4-abiraterone clearly better suppresses PSA, TMPRSS2 and FKBP5 expression in LNCAP, LAPC4 and C4-2 cell lines. D4-abiraterone also inhibits AR target gene expression in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo D4-abiraterone (D4A) is tenfold more potent than abiraterone (Abi) in blocking conversion from dehydroepiandrosterone (DHEA) by 3β-hydroxysteroid dehydrogenase (3βHSD) to D4-androstenedione (AD) in LNCaP and VCaP xenografts. 0.1 μM D4-abiraterone is equivalent to 1 μM Abi for blocking AD accumulation at 48 h in both LNCaP and VCaP xenografts. Progression is significantly delayed in the D4-abiraterone group compare with the Abi acetate group (P=0.011). D4-abiraterone treatment increases progression-free survival compare with Abi acetate . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CYP17A1, 3βHSD, SRD5A, androgen receptor |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC=C4C5=CN=CC=C5)C |
| PubChem CID | 196941 |
| 分子量 | 347.49 |
| RIDADR | NONHforallmodesoftransport |
|---|
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