计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
Information
Dutasteride Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).
In vitro
Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. Dutasteride is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. Dutasteride inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. Dutasteride also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. Dutasteride competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. Dutasteride (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. Dutasteride reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. Dutasteride results in overexpressed genes included genes encoding for proteins involved in biosynthesis and metabolism of androgen (HSD17B1;HSD17B3;CYP11B2), androgen receptor and androgen receptor co-regulators (AR;CCND1), and signal transduction(ERBB2; V-CAM; SOS1) whereas, underexpressed genes (KLK3; KLK2; DHCR24) are androgen-regulated genes (ARGs) in androgen-responsive (LNCaP) cell. Dutasteride inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells.
In vivo
Dutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. Dutasteride is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
度他雄胺
英文别名
(4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Dutasteride
生化机理
度他雄胺（GI198745，GG-745）是一种双重 5-α 还原酶抑制剂，可抑制睾酮向双氢睾酮（DHT）的转化。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
类固醇 5-α-还原酶抑制剂
名称和识别符
EC号
638-758-5
分子类型
小分子
Isomeric SMILES
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)NC4=C(C=CC(=C4)C(F)(F)F)C(F)(F)F)CC[C@@H]5[C@@]3(C=CC(=O)N5)C
分子量
528.53
Reaxy-Rn
24888215
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24888215&ln=
高级数据
产品属性
| ALogP | 5.4 |
|---|
关联靶点（人）
SRD5A1
Tclin
3-氧代-5-α-类固醇4-脱氢酶1(3-oxo-5-alpha-steroid 4-dehydrogenase 1)
(1 活性数据)
GLRA1
Tclin
甘氨酸受体亚基 α-1(Glycine receptor subunit alpha-1)
(1 活性数据)
化学和物理性质
熔点
246.0 to 250.0 °C
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
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危险品化学品经营许可证（带存储）