产品说明
应用
BAY 73-6691 has been used as a phosphodiesterase 9 inhibitor in ischemic heart samples and in structural studies. It may be used as a PDE 9 inhibitor in neuroblastoma SH-SY5Y cells.
包装
5, 25 mg in glass bottle
生化/生理作用
BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†
特点和优势
This compound is featured on the Phosphodiesterases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
基本信息
| 经验(实验)分子式 | C15H12ClF3N4O |
| 分子量 | 356.73 |
| MDL编号 | MFCD08705319 |
| PubChem化学物质编号 | 24724419 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | off-white |
| 溶解性 | DMSO: >20 mg/mL |
| 创始人 | Bayer |
| 储存温度 | 2-8℃ |
| SMILES string | C[C@H](CC1=Nc2c(cnn2-c3ccccc3Cl)C(=O)N1)C(F)(F)F |
| InChI | 1S/C15H12ClF3N4O/c1-8(15(17,18)19)6-12-21-13-9(14(24)22-12)7-20-23(13)11-5-3-2-4-10(11)16/h2-5,7-8H,6H2,1H3,(H,21,22,24)/t8-/m1/s1 |
| InChI key | FFPXPXOAFQCNBS-MRVPVSSYSA-N |
安全信息
| 象形图 |  |
| 警示用语： | Danger |
| 危险声明 | H300 - H315 - H319 - H335 - H413 |
| 预防措施声明 | P273 - P301 + P310 + P330 - P302 + P352 - P305 + P351 + P338 |
| 危险分类 | Acute Tox. 2 Oral - Aquatic Chronic 4 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3 |
| 靶器官 | Respiratory system |
| 储存分类代码 | 6.1B - Non-combustible, acute toxic Cat. 1 and 2 / very toxic hazardous materials |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
| 个人防护装备 | Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges |
