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Purity: ≥98%
Nilvadipine (formerly ARC-029; FR34235, FK235; ARC029; FR-34235; FK-235; Escor, Nivadil) is a potent calcium channel blocker (CCB) with potential antihypertensive activity. It has been used to treat chronic major cerebral artery occlusion and hypertension. Its IC50 is 0.03 NM, which indicates that it inhibits the calcium channel. In rat aortic smooth muscle cells (SMC), nilvadipine exhibits a strong chemotaxis-inhibiting effect on interleukin-1 (IL-1), leukotriene B4 (LTB4), and platelet-derived growth factor (PDGF), with an IC50 of 0.1 nM. It has been observed that nilvadipine increases renal blood flow and decreases the filtration fraction in the isolated perfused kidney of a hydronephrotic patient, which may indicate afferent and efferent arteriolar vasodilation indirectly.
| Targets |
Calcium channel ( IC50 = 0.1 nM )
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| ln Vivo |
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| Animal Protocol |
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| References |
| Molecular Formula |
C19H19N3O6
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| Molecular Weight |
385.37
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| Exact Mass |
385.13
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| Elemental Analysis |
C, 59.22; H, 4.97; N, 10.90; O, 24.91
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| CAS # |
75530-68-6
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| Related CAS # |
Nilvadipine-d4
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(C(=C(N1)C#N)C(=O)OC)C2=CC(=CC=C2)[N+](=O)[O-])C(=O)OC(C)C
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| InChi Key |
FAIIFDPAEUKBEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N3O6/c1-10(2)28-19(24)15-11(3)21-14(9-20)17(18(23)27-4)16(15)12-6-5-7-13(8-12)22(25)26/h5-8,10,16,21H,1-4H3
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| Chemical Name |
3-O-methyl 5-O-propan-2-yl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
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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 |
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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: ≥ 3.33 mg/mL (8.64 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 33.3 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: 3.33 mg/mL (8.64 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 33.3 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: ≥ 3.33 mg/mL (8.64 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 | 2.5949 mL | 12.9745 mL | 25.9491 mL | |
| 5 mM | 0.5190 mL | 2.5949 mL | 5.1898 mL | |
| 10 mM | 0.2595 mL | 1.2975 mL | 2.5949 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 |
| NCT02017340 | Completed | Drug: Nilvadipine Drug: Placebo |
Alzheimer's Disease | Prof Brian Lawlor | April 24, 2013 | Phase 3 |
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Products are for research use only; We do not sell to patients
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