Bioactivity | BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model[1][2][3]. |
Target | Soluble guanylate cyclase (sGC) |
Invitro | BAY-747 (100 nM) 与 WS 组合使用,可增强体外采集样 cLTP 模型中 AMPA 受体动力学[1] 。 Western Blot Analysis[1] Cell Line: |
In Vivo | BAY-747 在研究的时间范围内显示出 0.6 ± 2.0 的脑血浆比,反映出 60% 的相对较高的脑渗透[1]。BAY-747(0.03-1.0 mg/kg,2 mL/kg;口服;在 24 小时间隔 OLT 中 T1 前 30 分钟)增强大鼠对象定位任务 (OLT) 模型中的长期记忆获取过程,并减弱 L -NAME 引起短期记忆障碍。 BAY-747 不影响海马体中含有 GluA1 的 AMPAR 动力学[1]。BAY-747(0.003-0.3 mg/kg;口服;单剂量)降低大鼠的血压,并且(3 mg/kg;口服;每天一次,持续 35 天)增加接受 l-NAME 处理的肾素的大鼠体重 转基因模型[2]。BAY-747(150 mg/kg 食物;口服;16 周)提高雄性 mdx/mTRG2 小鼠的握力和跑步速度,表明骨骼肌功能得到改善[3]。 Animal Model: |
Name | BAY-747 |
CAS | 1609342-18-8 |
Formula | C22H26F2N4O2 |
Molar Mass | 416.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Nelissen E, et al. The sGC stimulator BAY-747 and activator runcaciguat can enhance memory in vivo via differential hippocampal plasticity mechanisms. Sci Rep. 2022 Mar 4;12(1):3589. [2]. Vakalopoulos A, et al. New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension. J Med Chem. 2023 Apr 11. [3]. Krishnan SM, et al. Assessing the Use of the sGC Stimulator BAY-747, as a Potential Treatment for Duchenne Muscular Dystrophy. Int J Mol Sci. 2021 Jul 27;22(15):8016. |