Bioactivity | ROMK-IN-32 is a renal outer medullary potassium channel (ROMK) inhibitor with an IC50 of 35 nM. ROMK-IN-32 also inhibits hERG with an IC50 of 22 μM[1]. |
Invitro | ROMK-IN-32 (compound 32) exhibits weak human SERT activity (IC50 10.4 μM; hSERT/hROMK EP=612x)[1]. |
In Vivo | 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]. |
Name | ROMK-IN-32 |
CAS | 1914944-54-9 |
Formula | C24H28N4O5 |
Molar Mass | 452.50 |
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]. Shuzhi Dong, et al. Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2559-2566. |