| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| E421099-1ml |
1ml |
现货  |
|
| 别名 | 伊那司他 (JTZ-951) |
|---|---|
| 英文别名 | C17H16N4O4 | Glycine, N-((7-hydroxy-5-(2-phenylethyl)(1,2,4)triazolo(1,5-a)pyridin-8-yl)carbonyl)- | JSK7TUA223 | UNII-JSK7TUA223 | Enarodustat (JTZ-951) | JTZ 951 | HY-109057 | BJ162590 | DB14985 | EX-A4798 | MS-25187 | 2-(7-Hydroxy-5-phenethyl-[1,2,4]tr |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Enarodustat (JTZ-951) |
| 生化机理 | Enarodustat (JTZ-951) 是一种强效口服活性 HIF 脯氨酰羟化酶抑制剂，对 PHD2 的 IC50 值为 0.22 μM，对 Hep3B 细胞 EPO 释放的 EC50 值为 5.7 μM。依那曲达具有治疗肾性贫血的潜力。 |
| 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 | Egl nine 同源物 1 抑制剂 |
| 产品介绍 |
Information Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia. Targets PHD2 (Cell-free assay); EPO release from Hep3B cells (Cell-based assay) 0.22 μM; 5.7 μM(EC50) In vitro Enarodustat (JTZ-951) inhibits PHD2 with IC50 of 0.22 μM and the EPO release from Hep3B cells with EC50 of 5.7 μM. In vivo JTZ-951 (compound 14), with a 5-phenethyl substituent on the triazolopyridine group, increases hemoglobin levels with daily oral dosing in rats. JTZ-951 is rapidly absorbed after oral administration and disappears shortly thereafter, which can be advantageous in terms of safety. JTZ-951 is selected as a clinical candidate. Cell Research(from reference) Cell lines：Hep3B cells Incubation Time：24 h |
| ALogP | 1.511 |
|---|---|
| hba_count | 4 |
| HBD Count | 2 |
| Rotatable Bond | 6 |
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 2-[[7-oxo-5-(2-phenylethyl)-3H-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]amino]acetic acid |
| INCHI | InChI=1S/C17H16N4O4/c22-13-8-12(7-6-11-4-2-1-3-5-11)21-16(19-10-20-21)15(13)17(25)18-9-14(23)24/h1-5,8,10H,6-7,9H2,(H,18,25)(H,19,20)(H,23,24) |
| InChi Key | FJYRBJKWDXVHHO-UHFFFAOYSA-N |
| Canonical SMILES | C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O |
| Isomeric SMILES | C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O |
| 分子量 | 340.33 |
| Reaxy-Rn | 50984607 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=50984607&ln= |
| DMSO(mg / mL) Max Solubility | 68 |
|---|---|
| DMSO(mM) Max Solubility | 199.806070578556 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 340.330 g/mol |
| XLogP3 | 1.600 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 6 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 340.117 Da |
| 单同位素质量Monoisotopic Mass | 340.117 Da |
| 拓扑极表面积Topological Polar Surface Area | 111.000 Ų |
| 重原子数Heavy Atom Count | 25 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 674.000 |
| 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 | 0 |
| 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 |
| Reaxy-Rn | 50984607 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=50984607&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
首页
400-620-6333
