| Size | Price | Stock | Qty |
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Purity: ≥98%
Nisoldipine (BAY-K-5552; Bay K-5552, Sular, Baymycard, Nisocor, Syscor) is a novel CCB-calcium channel blocker of the dihydropyridine (DHP) class with vasodilating and antihypertensive effects. It acts as a potent and specific blocker/inhibitor for L-type Cav1.2 with IC50 of 10 nM. Nisoldipine is used as a potent arterial vasodilator and antihypertensive agent. Nisoldipine is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels, which inhibits IKr (rapidly activating delayed-rectifier K+ current) with IC50 of 23 μM, and IKs (slowly activating delayed-rectifier K+ current) with IC50 of 40 μM in guinea-pig ventricular myocytes.
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| References |
| Molecular Formula |
C20H24N2O6
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| Molecular Weight |
388.41
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| CAS # |
63675-72-9
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| Related CAS # |
Nisoldipine-d6;1285910-03-3;Nisoldipine-d4;1219795-47-7;Nisoldipine-d7;1189718-34-0
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| SMILES |
O(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])[H])C1([H])C1=C([H])C([H])=C([H])C([H])=C1[N+](=O)[O-])=O
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| InChi Key |
VKQFCGNPDRICFG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3
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| Chemical Name |
3-isobutyl 5-methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.44 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 (6.44 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5746 mL | 12.8730 mL | 25.7460 mL | |
| 5 mM | 0.5149 mL | 2.5746 mL | 5.1492 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5746 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00979537 | Completed | Drug: Nisoldipine Extended-release Tablets, 40 mg |
Healthy | Mylan Pharmaceuticals Inc | March 2007 | Phase 1 |
| NCT00985660 | Completed | Drug: Nisoldipine Extended-release Tablets, 30 mg |
Healthy | Mylan Pharmaceuticals Inc | June 2007 | Phase 1 |
| NCT00730197 | Completed | Drug: Albuterol Sulfate Extended- Release Tablets 8 mg |
Healthy | Mylan Pharmaceuticals Inc | February 2007 | Phase 1 |
| NCT00311870 | Completed | Drug: nisoldipine Drug: lisinopril |
Diabetic Nephropathy | Steno Diabetes Center Copenhagen | March 1993 | Phase 4 |
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