Osilodrostat phosphate, 细胞色素 P450 11B1 抑制剂

COA

级别和纯度:

≥99%

CAS编号: 1315449-72-9
分子式: C₁₃H₁₃FN₃O₄P
分子量: 325.23
PubChem编号: 71009737

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货号 (SKU)	包装规格	是否现货
O648722-5mg	5mg	期货
O648722-10mg	10mg	期货
O648722-25mg	25mg	期货
O648722-50mg	50mg	期货
O648722-100mg	100mg	期货

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Glucose Metabolism (3713) Metabolic Enzyme/Protease (4889) Mineralocorticoid Receptor (19) Vitamin D Related/Nuclear Receptor (908)

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基本描述

别名	磷酸奥司他
英文别名	Osilodrostat phosphate \| Q27294304 \| CHEMBL3707393 \| Osilodrostat (phosphate) \| AKOS040749099 \| Osilodrostat phosphate [USAN] \| Osilodrostat phosphate (JAN/USAN) \| Isturisa (TN) \| D11062 \| UNII-Y6581YAW9V \| DTXSID401027857 \| 4-[(5R)-6,7-dihydro-5H-pyrrolo
规格或纯度	≥99%
英文名称	Osilodrostat phosphate
生化机理	Osilodrostat（LCI699）磷酸盐是一种强效的口服活性 11β-hydroxylase (CYP11B1) 抑制剂，IC 50 值为 35 nM。Osilodrostat 磷酸酯是一种强效的口服醛固酮合成酶（CYP11B2）抑制剂，对人类和哺乳动物的 IC 50 值分别为 0.7 nM 和 160 nM。
储存温度	2-8°C储存,干燥
运输条件	冰袋运输
作用类型	抑制剂
作用机制	细胞色素 P450 11B1 抑制剂
产品介绍	Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC 50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC 50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS) In Vitro Osilodrostat (LCI699; 0.01-10 µM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells) phosphate inhibits cortisol and aldosterone. Osilodrostat results in inhibition of corticosterone, 11-deoxycortisol accumulation, and modest effects on adrenal androgens. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) phosphate inhibits aldosterone and corticosterone synthesis in Ang-II- and ACTH-stimulated Sprague Dawley rats . Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) phosphate reduces mean arterial pressure and prolongs survival in dTG rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Ang-II- and ACTH-stimulated Sprague Dawley rats Dosage: 0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats) Administration: Oral administration; once Result: Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner. Animal Model: dTG rats Dosage: 3, 10, 30 and 100 mg/kg Administration: Oral administration; daily, for 52 weeks Result: Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner. Form:Solid IC50& Target:IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)
纯度	≥99%

名称和识别符

分子类型	小分子
IIUPAC Name	4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile;phosphoric acid
INCHI	1S/C13H10FN3.H3O4P/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13;1-5(2,3)4/h1,3,5,7-8,13H,2,4H2;(H3,1,2,3,4)/t13-;/m1./s1
InChi Key	FMCPYRDGUZBOJZ-BTQNPOSSSA-N
Smiles	C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F.OP(=O)(O)O
Isomeric SMILES	C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F.OP(=O)(O)O
PubChem CID	71009737
分子量	325.23

化学和物理性质

溶解性	H2O : ≥ 200 mg/mL (614.95 mM)
分子量	325.230 g/mol
XLogP3
氢键供体数Hydrogen Bond Donor Count	3
氢键受体数Hydrogen Bond Acceptor Count	7
可旋转键计数Rotatable Bond Count	1
精确质量Exact Mass	325.063 Da
单同位素质量Monoisotopic Mass	325.063 Da
拓扑极表面积Topological Polar Surface Area	119.000 Å²
重原子数Heavy Atom Count	22
形式电荷Formal Charge	0
复杂度Complexity	387.000
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	2

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