BAY 73-6691

• 产品号: B3561
• CAS号: 794568-92-6
• 分子式: C15H12ClF3N4O
• 分子量: 356.7301896
• 纯 度: ≥98% (HPLC)

产品别名

• 标题: BAY 73-6691
• IUPAC标准名: 1-(2-chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1H,4H,5H-pyrazolo[3,4-d]pyrimidin-4-one
• IUPAC传统名: 1-(2-chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-5H-pyrazolo[3,4-d]pyrimidin-4-one
• 别名: 1-(2-Chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one

产品登记号

• CAS号: 794568-92-6
• MDL号: MFCD08705319
• PubChem SID: 24724419

产品性质

• Empirical Formula (Hill Notation): C15H12ClF3N4O
• 纯度: ≥98% (HPLC)
• 外观: off-white powder
• 溶解度: DMSO: >20 mg/mL
• GHS警示词: Danger
• GHS危险声明: H300-H315-H319-H335-H413
• 欧盟危险性物质标志: 有毒(Toxic) (T)
• 欧盟危险性物质标志: 刺激性(Irritant) (Xi)
• 个人保护装置: Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
• GHS警示性声明: P261-P264-P301 + P310-P305 + P351 + P338
• RID/ADR: UN 2811 6.1/PG 3
• 危险公开号: 25-36/37/38
• 安全公开号: 26-45
• 保存温度: 2-8°C
• 联合国危险货物等级: 6.1
• 联合国危险货物编号: 2811
• 联合国危险货物包装类别(PG): 3
• 德国WGK号: 3

产品详细信息

详细说明 (English)

Biochem/physiol Actions
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.†

详细说明 (简体中文)

Biochem/physiol Actions
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.†