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) |
|---|
概述
Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor ( GR ) modulator with a K i value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders
In Vitro
In HepG2 human cells or in human hepatocytes, Dazucorilant acts as full antagonist since it is able to prevent the dexamethasone-induced increase in TAT activity and to induce non-measurable agonist activity in the absence of dexamethasone. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity . Dazucorilant (5, 10 or 20 mg/kg; i.p.) reverses hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restores the hippocampal levels of synaptic markers, reestablishes basal plasma levels of glucocorticoids and improves cognitive function at a dose of 10 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Wobbler mice (five-month-old) Dosage: 30 mg/kg/day Administration: S.c. Result: Wobbler mice showed reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity. Animal Model: Adult SD male ratsDosage: 5, 10 or 20 mg/kg Administration: I.p. Result: Reversed hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restored the hippocampal levels of synaptic markers, reestablished basal plasma levels of glucocorticoids and improved cognitive function at a dose of 10 mg/kg.
Form:Solid
IC50& Target:GR
规格
别名
达克宁
英文名称
Dazucorilant
生化机理
Dazucorilant（CORT113176）是一种选择性高亲和力非类固醇糖皮质激素受体（GR）调节剂，体外 K i 值＜1 nM。Dazucorilant 可用于神经系统疾病的研究。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
调节剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CN(C[C@@]2(C1=CC3=C(C2)C=NN3C4=CC=C(C=C4)F)C(=O)C5=CC=CC=N5)S(=O)(=O)C6=CC=C(C=C6)C(F)(F)F
PubChem CID
分子量
582.57
高级数据
关联靶点（人）
NR3C1
Tclin
糖皮质激素受体(Glucocorticoid receptor)
(5 活性数据)
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(1 活性数据)
NR3C1
Tclin
Glucocorticoid receptor
(14987 活性数据)
KCNH2
Tclin
HERG
(29587 活性数据)
关联靶点（其它种属）
Rattus norvegicus (775804 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
分子量
582.600 g/mol
XLogP3
4.600
氢键供体数Hydrogen Bond Donor Count
0
氢键受体数Hydrogen Bond Acceptor Count
10
可旋转键计数Rotatable Bond Count
5
精确质量Exact Mass
582.135 Da
单同位素质量Monoisotopic Mass
582.135 Da
拓扑极表面积Topological Polar Surface Area
93.500 Ų
重原子数Heavy Atom Count
41
形式电荷Formal Charge
0
复杂度Complexity
1110.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
1
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
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
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）