| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In dog ventricular myocytes, concentration-dependent reduction of NCX currents is observed with ORM-10962 (10 nM, 100 nM, and 1 μM), with estimated IC50 values of 55 and 67 nM mV at -80 and 20 mV, respectively [1].
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| ln Vivo |
In anesthetized guinea pigs, the administration of ORM-10962 (0.3 mg/kg, IV, once) markedly postpones the onset of anesthesia and premature ventricular contractions (about 50%) or ventricular tachycardia (about 30%) [1].
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| Animal Protocol |
Animal/Disease Models: Male guinea pigs (250-300 g) [1]
Doses: 0.3 mg/kg Route of Administration: intravenous (iv) (iv)injection, 10 minutes before starting ouabain infusion Experimental Results: Significant delay in the development of premature ventricular contractions (from 24 in the control group ±1.7 minutes to 36.6±2.7 minutes in the presence of drug) or ventricular tachycardia (from 31.8±1.8 minutes in the control group to 40.8±2.1 minutes in the presence of drug). |
| References |
|
| Molecular Formula |
C27H29N3O4
|
|---|---|
| Molecular Weight |
459.5369
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| Exact Mass |
459.215
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| CAS # |
763926-98-3
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| PubChem CID |
69016811
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
650
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C(N([H])C2=C([H])N=C(C([H])=C2[H])OC2C([H])=C([H])C3=C(C=2[H])C([H])([H])C([H])([H])C([H])(C2C([H])=C([H])C([H])=C([H])C=2[H])O3)=O)C([H])([H])C1([H])[H]
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| InChi Key |
UPGUBLDTYLMRHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29N3O4/c31-22-12-14-30(15-13-22)18-26(32)29-21-7-11-27(28-17-21)33-23-8-10-25-20(16-23)6-9-24(34-25)19-4-2-1-3-5-19/h1-5,7-8,10-11,16-17,22,24,31H,6,9,12-15,18H2,(H,29,32)
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| Chemical Name |
2-(4-hydroxypiperidin-1-yl)-N-[6-[(2-phenyl-3,4-dihydro-2H-chromen-6-yl)oxy]pyridin-3-yl]acetamide
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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 : ~250 mg/mL (~544.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.53 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 20.8 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: ≥ 2.08 mg/mL (4.53 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 20.8 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: ≥ 2.08 mg/mL (4.53 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 | 2.1761 mL | 10.8804 mL | 21.7609 mL | |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3522 mL | |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1761 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.
Products are for research use only; We do not sell to patients
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