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Osilodrostat (LCI699), CYP11B1 抑制剂;CYP11B2 抑制剂

P450（例如CYP17）抑制剂
COA COA
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货号 (SKU) 包装规格 是否现货 价格 数量
O413758-2mg
 2mg 现货 Stock Image
O413758-5mg
 5mg 现货 Stock Image
O413758-10mg
 10mg 现货 Stock Image
O413758-25mg
 25mg 现货 Stock Image
O413758-50mg
 50mg 现货 Stock Image
O413758-100mg
 100mg 现货 Stock Image
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查看相关系列
CYP11B1 Inhibitor (5) CYP11B2 Inhibitor (2) 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 奥西洛司他 (LCI699)
英文别名 (R)-4-(6,7-Dihydro-5H-pyrrolo(1,2-c)imidazol-5-yl)-3-fluorobenzonitrile | GTPL8310 | 5YL4IQ1078 | OSILODROSTAT [WHO-DD] | Osilodrostat free base | Osilodrostat;4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile | TRICLOCARBAN (USP MO
规格或纯度 Moligand™, ≥99%
英文名称 Osilodrostat (LCI699)
生化机理 LCI699（奥西洛前列素）是一种强效的 11β- 羟化酶（CYP11B）抑制剂，这种酶催化皮质醇合成的最后一步。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 CYP11B1 抑制剂;CYP11B2 抑制剂
产品介绍


Information

Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B) , an enzyme catalyzing the final step of cortisol synthesis.


Targets

11β-hydroxylase 2.5 nM


In vitro

LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1.


In vivo

LCI699 is a potent inhibitor of 11β-hydroxylase (CYP11B1), the enzyme that catalyzes the final step of cortisol synthesis, and has a half-life of ∼4 hours. It decreases blood pressure (BP) in patients with essential hypertension and primary aldosteronism. Treatment with LCI699 is well tolerated, it is demonstrated efficacy with a satisfactory safety and tolerability profile in the proof-of-concept study in Cushing\'s disease. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism.
纯度 ≥99%

产品属性

ALogP 2.02
hba_count 1
Rotatable Bond 1

关联靶点（人）

CYP11B2 Tchem 细胞色素 P450 11B2，线粒体(Cytochrome P450 11B2, mitochondrial) (12 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP11B1 Tclin 细胞色素 P450 11B1，线粒体(Cytochrome P450 11B1, mitochondrial) (9 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP19A1 Tclin 芳香化酶(Aromatase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP19A1 Tclin Cytochrome P450 19A1 (6099 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP11B1 Tclin Cytochrome P450 11B1 (1750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD4 Tchem Dopamine D4 receptor (7907 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM4 Tclin Muscarinic acetylcholine receptor M4 (6041 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM5 Tclin Muscarinic acetylcholine receptor M5 (4677 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD5 Tchem Dopamine D5 receptor (1597 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EDNRB Tclin Endothelin receptor ET-B (1928 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TACR1 Tclin Neurokinin 1 receptor (6273 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TACR2 Tchem Neurokinin 2 receptor (3341 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABBR1 Tclin GABA-B receptor 1 (184 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Htr7 Serotonin 7 (5-HT7) receptor (19 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ntsr1 Neurotensin receptor 1 (48 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Bdkrb1 Bradykinin B1 receptor (77 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cyp11b2 Cytochrome P450 11B2 (46 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE6A Phosphodiesterase 6A (40 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cynomolgus monkey (4946 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cyp11b2 Cytochrome P450 11B2, mitochondrial (28 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

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

名称和识别符

PubChem SID 504770281
分子类型 小分子
IIUPAC Name 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
INCHI 1S/C13H10FN3/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13/h1,3,5,7-8,13H,2,4H2/t13-/m1/s1
InChi Key USUZGMWDZDXMDG-CYBMUJFWSA-N
Smiles C1CC2=CN=CN2C1C3=C(C=C(C=C3)C#N)F
Isomeric SMILES C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F
分子量 227.24
Reaxy-Rn 11722147
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11722147&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 45 mg/mL (198.02 mM); Ethanol: 45 mg/mL (198.02 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 45
DMSO(mM) Max Solubility 198.0285161
Water(mg / mL) Max Solubility 15
Water(mM) Max Solubility 66.00950537
分子量 227.240 g/mol
XLogP3 1.900
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 3
可旋转键计数Rotatable Bond Count 1
精确质量Exact Mass 227.086 Da
单同位素质量Monoisotopic Mass 227.086 Da
拓扑极表面积Topological Polar Surface Area 41.600 Ų
重原子数Heavy Atom Count 17
形式电荷Formal Charge 0
复杂度Complexity 337.000
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

安全和危险性（GHS）

象形图 GHS07
信号词 警告
危险声明

H302: 吞食有害

H315: 引起皮肤刺激

H320: 引起眼睛刺激

H335: 可能引起呼吸道刺激
预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。

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找到6个结果

批号(Lot Number) 证书类型 货号
K2228505 分析证书 O413758
K2228506 分析证书 O413758
K2228507 分析证书 O413758
K2228508 分析证书 O413758
K2228509 分析证书 O413758
K2228710 分析证书 O413758

引用文献

1. Amar L, Azizi M, Menard J, Peyrard S, Watson C, Plouin PF.  (2010)  Aldosterone synthase inhibition with LCI699: a proof-of-concept study in patients with primary aldosteronism..  Hypertension,  56  (5): (831-8).  [PMID:20837883]
2. Calhoun DA, White WB, Krum H, Guo W, Bermann G, Trapani A, Lefkowitz MP, Ménard J.  (2011)  Effects of a novel aldosterone synthase inhibitor for treatment of primary hypertension: results of a randomized, double-blind, placebo- and active-controlled phase 2 trial..  Circulation,  124  (18): (1945-55).  [PMID:21986283]
3. Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW.  (2014)  Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors..  J Med Chem,  57  (12): (5179-89).  [PMID:24899257]
4. Fleseriu M, Petersenn S.  (2015)  Medical therapy for Cushing's disease: adrenal steroidogenesis inhibitors and glucocorticoid receptor blockers..  Pituitary,  18  (2): (245-52).  [PMID:25560275]
5. Daniel E, Newell-Price JD.  (2015)  Therapy of endocrine disease: steroidogenesis enzyme inhibitors in Cushing's syndrome..  Eur J Endocrinol,  172  (6): (R263-80).  [PMID:25637072]
6. Wang HZ, Tian JB, Yang KH.  (2015)  Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review..  Eur Rev Med Pharmacol Sci,  19  (2): (296-304).  [PMID:25683946]
7. Fleseriu M.  (2015)  Medical Treatment of Cushing Disease: New Targets, New Hope..  Endocrinol Metab Clin North Am,  44  (1): (51-70).  [PMID:25732642]
8. Duggan S.  (2020)  Osilodrostat: First Approval..  Drugs,  80  (5): (495-500).  [PMID:32141023]

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