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说明： Potent and selective ROCK2 inhibitor; orally bioavailable and brain penetrant
化学名： (2R)-4-(3-Fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-1-piperazinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for CHDI 00580985
CHDI 00580985 is a potent and selective ROCK inhibitor (IC50 values are 3 nM and 8 nM in biochemical (ROCK2) and cellular assays respectively). CHDI 00580985 inhibits ROCK-mediated substrate (MYPT1) phosphorylation (IC50 = 4 nM). In vivo, CHDI 00580985 reduces ROCK signaling in Huntington's disease mouse models in pharmacodynamic assay. CHDI 00580985 is bioavailable and brain penetrant.
许可信息
Sold under license from CHDI Foundation
技术数据 for CHDI 00580985
| 分子量 | 372.44 |
| 公式 | C20H25FN4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2573071-18-6 |
| PubChem ID | 155749520 |
| InChI Key | CIPXFTLGPVQJKN-HUUCEWRRSA-N |
| Smiles | FC1=CN=CC=C1N2C[C@H](N(CC2)C(N[C@@H](C3=CC(OC)=CC=C3)C)=O)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CHDI 00580985
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 37.24 | 100 | |
| ethanol | 37.24 | 100 |
制备储备液 for CHDI 00580985
以下数据基于产品分子量 372.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.68 mL | 13.42 mL | 26.85 mL |
| 5 mM | 0.54 mL | 2.68 mL | 5.37 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.68 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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产品说明书 for CHDI 00580985
参考文献 for CHDI 00580985
参考文献是支持产品生物活性的出版物。
Ladduwahetty et al (2022) Identification of a potent, selective, and brain-penetrant Rho kinase inhibitor and its activity in a mouse model of Huntington's disease. J.Med.Chem. 65 9819 PMID: 35816678
If you know of a relevant reference for CHDI 00580985, please let us know.
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关键词: CHDI 00580985, CHDI 00580985 supplier, CHDI00580985, potent, selective, ROCK, inhibitors, inhibits, ROCK1, ROCK2, in, vivo, orally, bioavailable, brain, penetrant, Huntington's, disease, Rho-kinases, 7881, Tocris Bioscience
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