2062661-53-2
2062661-53-2 structure
- Name: Tovinontrine
- Chemical Name: Tovinontrine
- CAS Number: 2062661-53-2
- Molecular Formula: C21H26N6O2
- Molecular Weight: 394.47
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
- Create Date: 2021-10-08 19:04:03
- Modify Date: 2024-01-10 18:29:30
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Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively[1].
| Name | Tovinontrine |
|---|
| Description | Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
PDE9A1:8.19 nM () PDE9A2:9.99 nM () PDE1A3:88.4 nM () PDE1B:8.48 nM () PDE1C:12.2 nM () PDE5A2:81.9 nM () |
| In Vitro | IMR-687 inhibits PDE9A with more than 800-fold greater potency than PDE1A3, PDE1B, PDE1C, PDE5A2, with IC50 values of 88.4 μM, 8.48 μM, 12.2 μM, and 81.9 μM, respectively[1]. IMR-687 (0.1-10 μM) treatment in erythroid K562 cells for 72 hours induces hemoglobin (HbF) in a dose-dependent manner[1]. IMR-687 (0.03-10 μM) treatment for 6 hours in erythroid K562 cells increases cGMP in a dose-dependent manner[1]. |
| In Vivo | IMR-687 (30 mg/kg/day; after 30 days of treatment) shows a greater than 3-fold in the percent of HbF+ F-cells (8.4% in vehicle treated and 27.3% in IMR-687 treated) and a corresponding 2-fold decrease in sickled red blood cells (56.3% in vehicle treated and 24.4% in IMR-687 treated)[1]. Animal Model: HbSS-Townes mice on a 129/B6 background (10-12 weeks old) [1] Dosage: 30 mg/kg Administration: Dosed daily by gavage for 30 days Result: Resulted in fetal hemoglobin (HbF) induction, reduced hemolysis and reduced reticulocytosis. |
| References |
| Molecular Formula | C21H26N6O2 |
|---|---|
| Molecular Weight | 394.47 |