ROMK-IN-32 是一种肾外髓质钾通道 (ROMK) 抑制剂,IC50为 35 nM. ROMK-IN-32 也抑制 HERG ,IC50为 22 μM。
产品描述
ROMK-IN-32 is a renal outer medullary potassium channel ( ROMK ) inhibitor with an IC 50 of 35 nM. ROMK-IN-32 also inhibits hERG with an IC 50 of 22 μM [1].
体外活性
ROMK-IN-32 (compound 32) exhibits weak human SERT activity (IC 50 10.4 μM; hSERT/hROMK EP=612x) [1].
体内活性
ROMK-IN-32 demonstrates blood pressure lowering effects in the spontaneously hypertensive rat model [1]. ROMK-IN-32 exhibits moderate oral bioavailability (78%) following oral administration (1 mg/kg) in WH rats [1]. ROMK-IN-32 exhibits terminal elimination half-lives (rat 4.7 and dog 5.8 h) due to high plasma clearance (9.6 and 18.3 mL/min/kg respectively) combined with large volumes of distribution (3.0 and 5.0 L/kg respectively) following intravenous administration (rat 0.5 and dog 1.0 mg/kg) [1].
Cas No.
1914944-54-9
分子式
C24H28N4O5
分子量
452.5
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years