1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Tovinontrine

Tovinontrine (Synonyms: IMR-687)

Cat. No.: HY-109193
Handling Instructions

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.

For research use only. We do not sell to patients.

Tovinontrine Chemical Structure

Tovinontrine Chemical Structure

CAS No. : 2062661-53-2

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

394.47

Formula

C₂₁H₂₆N₆O₂

CAS No.
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Please store the product under the recommended conditions in the Certificate of Analysis.

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Tovinontrine
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HY-109193
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