| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| O426958-1ml |
1ml |
现货  |
|
| 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™, 10mM in DMSO |
| 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 | -80℃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. |
| ALogP | 2.02 |
|---|---|
| hba_count | 1 |
| Rotatable Bond | 1 |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile |
| INCHI | 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 |
| Canonical 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= |
| 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 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害 |
| 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。 |
| Reaxy-Rn | 11722147 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11722147&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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