Nitrendipine [39562-70-4]
Référence NB-64-00260-50mg
Conditionnement : 50mg
Marque : Neo Biotech
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Nitrendipine
(Synonyms: Bayotensin, BAY-E-5009) Copy Product InfoSynonyms: Bayotensin, BAY-E-5009
Catalog No. T0119 Copy Product Info
Purity: 99.55%
Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.
Cas No. 39562-70-4
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.55%
Appearance:Solid
Color:White
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Product Information
Nitrendipine AI Summary
Nitrendipine exhibits a wide range of bioactivities across multiple biological systems and potential therapeutic areas. It demonstrates significant inhibitory effects on calcium channels, particularly the L-type calcium channels with extremely low IC50 values (as low as 0.35 nM). This suggests potent activity as a calcium channel blocker, which translates to potential vasorelaxant properties in vascular tissues, evidenced by a reported IC50 of 1.0 nM in rabbit thoracic aorta and EC50 of 30.0 nM in rat endothelium-denuded thoracic aortic rings. Additionally, Nitrendipine shows significant antihypertensive effects in SHR rats, reducing both systolic and diastolic blood pressure. In hepatic metabolism, Nitrendipine inhibits cytochrome P-450 enzymes, with substantial inhibition rates reported, such as 83.0% inhibition on human liver microsomes. This suggests potential interactions affecting drug metabolism. The compound also exhibits notable partition characteristics (CLogP of 3.16 and logD of 0.97), indicating moderate lipophilicity and ability to permeate cellular membranes, though it has low permeability across Caco-2 cells. While Nitrendipine effectively inhibits sodium channels and shows an antifungal effect, it also exhibits moderate to weak activity against adenosine receptors and displays diverse bioactivity against Plasmodium falciparum, suggesting antimalarial potential. The compound shows a broad range of inhibitory effects on other targets, including the SARS-CoV-2 virus and various transporters and enzymes within cellular systems, highlighted by high clearance rates in hepatic metabolism and significant protein binding properties. However, observations of moderate liver toxicity and potential nephrotoxic effects highlight the need for further safety evaluations. Additionally, the compound's low oral bioavailability suggests limitations in its systemic availability when administered orally. Overall, Nitrendipine demonstrates a rich pharmacological profile with significant activities in modulating calcium channels, cytochrome P-450 enzymes, antiviral properties against SARS-CoV-2, as well as potential cardiovascular effects, meriting further investigation for therapeutic development while considering safety and bioavailability aspects..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. |
| Targets & IC50 | Ca2+ channel:95 nM |
| Synonyms | Bayotensin, BAY-E-5009 |
| Molecular Weight | 360.36 |
| Formula | C18H20N2O6 |
| Cas No. | 39562-70-4 |
| Smiles | C(OCC)(=O)C=1C(C(C(OC)=O)=C(C)NC1C)C2=CC(N(=O)=O)=CC=C2 |
| Relative Density. | 1.3595 g/cm3 (Estimated) |
| Storage | Keep away from direct sunlight, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||
| Solubility Information | DMSO: 247.5 mg/mL (686.81 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (27.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (27.75 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||
DMSO
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