| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
IMR-687 has an inhibitory efficacy of about 800 times greater than PDE9A, PDE1A3, PDE1B, PDE1C, and PDE5A2, with IC50 values of 88.4 μM, 8.48 μM, 12.2 μM, and 81.9 μM, in that order [1]. Hemoglobin (HbF) is generated in K562 cells for 72 hours in red blood cells by IMR-687 (0.1–10 μM) in a dose-dependent manner [1]. In erythroid K562 cells, IMR-687 (0.03-10 μM) raises cGMP in a dose-dependent manner over a 6-hour period [1].
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| ln Vivo |
IMR-687 (30 mg/kg/day; after 30 days of therapy) demonstrated a more than 3-fold rise in the percentage of HbF+ F cells (vehicle treatment: 8.4%, IMR-687 treatment: 27.3%) and a similar 2-fold reduction in sickle red cells ( Carrier treatment: 56.3% and IMR-687 treatment: 24.4%)[1].
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| Animal Protocol |
Animal/Disease Models: HbSS-Townes mice (10-12 weeks old) on 129/B6 background [1]
Doses: 30 mg/kg Route of Administration: Dosage daily gavage for 30 days Experimental Results: Caused fetal hemoglobin (HbF) induction, diminished hemolysis, and increased reticulocytosis. |
| References |
[1]. James G McArthur, et al. A novel, highly potent and selective phosphodiesterase-9 inhibitor for the treatment of sickle cell disease. Haematologica. 2020 Mar;105(3):623-631.
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| Molecular Formula |
C21H26N6O2
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|---|---|
| Molecular Weight |
394.48
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| Exact Mass |
394.21
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| Elemental Analysis |
C, 63.94; H, 6.64; N, 21.30; O, 8.11
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| CAS # |
2062661-53-2
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| SMILES |
O=C1C2=CN=C(C3CCOCC3)N2C=C([C@@H]4CN(CC5=NC=CC=N5)C[C@H]4C)N1
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| InChi Key |
GWGNPYYVGANHRJ-GDBMZVCRSA-N
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| InChi Code |
InChI=1S/C21H26N6O2/c1-14-10-26(13-19-22-5-2-6-23-19)11-16(14)17-12-27-18(21(28)25-17)9-24-20(27)15-3-7-29-8-4-15/h2,5-6,9,12,14-16H,3-4,7-8,10-11,13H2,1H3,(H,25,28)/t14-,16-/m1/s1
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| Chemical Name |
6-{(3S,4S)-4-methyl-1-[(pyrimidin-2-yl)methyl]pyrrolidin-3-yl}-3-(oxan-4-yl)imidazo[1,5-a]pyrazin-8(7H)-one
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| Synonyms |
Tovinontrine; IMR-687; IMR 687; IMR687;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~253.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5350 mL | 12.6749 mL | 25.3498 mL | |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0700 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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