MK-0773

• 常用名: MK-0773
• 英文名: MK-0773
• CAS号: 606101-58-0
• 分子量: 479.590
• 密度: 1.3±0.1 g/cm3
• 沸点: 754.2±60.0 °C at 760 mmHg
• 分子式: C₂₇H₃₄FN₅O₂
• 熔点: N/A
• 闪点: 409.9±32.9 °C

MK-0773用途

MK-0773 是一种选择性雄激素受体调节剂 (selective androgen receptor modulators),与 AR 结合,IC50 值为 6.6 nM。

MK-0773名称

• 中文名: MK-0773
• 英文名: (1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide

MK-0773生物活性

• 描述: MK-0773 是一种选择性雄激素受体调节剂 (selective androgen receptor modulators),与 AR 结合,IC50 值为 6.6 nM。
• 相关类别:
  信号通路 >> 其他 >> 雄激素受体
  研究领域 >> 内分泌
• 靶点实验:

  IC50: 6.6 nM (AR)

• 体外研究: MK-0773与AR结合的IC50在25％大鼠血清存在下增加3.5倍,在25％人血清存在下增加13倍,表明它与血清蛋白结合。使用转染AR的COS细胞评估MK-0773对AR跨物种的亲和力,并且IC50值在四个物种(大鼠,0.50nM;狗,0.55nM;恒河猴,0.45nM;人,0.65nM)中非常相似[ 1]。
• 体内研究: MK-0773(6和80mg/kg,sc)在OVX大鼠模型中对皮质BFR和LBM产生暴露相关的刺激作用。 MK-0773(5,15和80mg/kg,sc)增加精囊重量,并且对前列腺的作用降低。 MK-0773的部分激动和组织选择性不会转化为对OVX大鼠脂质代谢的不同影响[1]。
• 动物实验: 大鼠：在睾丸切除术（ORX）后，在3-4个月大的250-300-g大鼠中研究前列腺和精囊。手术后9天，每天给动物注射（皮下）试验化合物17天，并将精囊（SVs）的重量与用载体或DHT作为阳性对照处理的ORX大鼠进行比较。
• 参考文献:

  [1]. Schmidt A, et al. Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology. J Biol Chem. 2010 May 28;285

MK-0773物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 754.2±60.0 °C at 760 mmHg
• 分子式: C₂₇H₃₄FN₅O₂
• 分子量: 479.590
• 闪点: 409.9±32.9 °C
• 精确质量: 479.269653
• PSA: 94.47000
• LogP: 3.17
• InChIKey: GBEUKTWTUSPHEE-JWJWXJQQSA-N
• SMILES: CN1C(=O)C(F)=CC2(C)C3CCC4(C)C(C(=O)NCc5nc6ncccc6[nH]5)CCC4C3CCC12
• 蒸汽压: 0.0±2.5 mmHg at 25°C
• 折射率: 1.632
• 储存条件: 2-8℃

MK-0773靶点实验

查看更多实验

实验名称：Androgenic activity in ORX rat model assessed as increase in prostate weight at 30 mg... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3222671

实验名称：Androgenic activity in ORX rat model assessed as increase in levator ani muscle weigh... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3222673

实验名称：Agonist activity at human AR expressed in African green monkey CV1 cells assessed as ... 来源：ChEMBL 靶标：Androgen receptor External Id：CHEMBL3222676

实验名称：Agonist activity at human AR expressed in African green monkey CV1 cells assessed as ... 来源：ChEMBL 靶标：Androgen receptor External Id：CHEMBL3222678

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Agonist activity at human AR expressed in African green monkey CV1 cells assessed as ... 来源：ChEMBL 靶标：Androgen receptor External Id：CHEMBL3222679

实验名称：Androgenic activity in ORX rat model assessed as increase in levator ani muscle weigh... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3222682

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

实验名称：Androgenic activity in ORX rat model assessed as increase in prostate weight at 3 mg/... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3222684

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

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MK-0773英文别名

• mk 0773
• (4aS,4bS,6aS,7S,9aS,9bS,11aR)-3-Fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-1,4a,6a-trimethyl-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
• unii-5730vnw22x
• MK-0773