| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Viquidil HCl targets voltage-gated calcium channels, particularly L-type calcium channels, in vascular smooth muscle cells. By binding to the α1 subunit of the calcium channel, Viquidil inhibits the influx of calcium ions into the cell, which is essential for muscle contraction. This inhibition leads to relaxation of vascular smooth muscle, vasodilation, and a reduction in blood pressure. The compound's selectivity for vascular smooth muscle over cardiac muscle contributes to its antihypertensive effects.
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| ln Vitro |
In vitro, Viquidil HCl has been shown to inhibit calcium influx in vascular smooth muscle cells and to relax pre-contracted arterial rings. The compound's vasodilatory effects are concentration-dependent and are mediated by the blockade of L-type calcium channels. In cell-based assays, Viquidil inhibits calcium-induced contraction of vascular smooth muscle cells with an IC₅₀ in the micromolar range. These in vitro findings are consistent with its mechanism of action as a calcium channel blocker.
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| ln Vivo |
In rabbits, quinixin hydrochloride, also known as quidil hydrochloride, has the ability to markedly enhance cerebral blood flow [3].
In vivo, Viquidil HCl has been shown to lower blood pressure in animal models of hypertension. The compound's vasodilatory effects lead to a reduction in peripheral vascular resistance and a decrease in blood pressure. Viquidil has been studied in clinical trials for the treatment of hypertension, although its clinical use is limited. The compound's efficacy and safety have been evaluated in preclinical and clinical studies. |
| Enzyme Assay |
In vitro receptor binding assays for Viquidil HCl involve measuring its binding affinity to voltage-gated calcium channels. The assay is typically performed using membrane preparations from cells expressing L-type calcium channels. Radiolabeled ligands, such as [³H]-nitrendipine, are used in competition binding assays. The compound is incubated with the receptor membranes and the radioligand, and the bound radioactivity is measured using a scintillation counter. The Ki values are calculated from the displacement curves.
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| Cell Assay |
In vitro cellular experiments for Viquidil HCl are performed using vascular smooth muscle cells. Cells are treated with varying concentrations of the compound, and the inhibition of calcium influx is assessed using fluorescent calcium indicators, such as Fura-2. The compound's effects on cell contraction are assessed using a cell contraction assay. These experiments are essential for characterizing the compound's functional activity as a calcium channel blocker.
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| Animal Protocol |
In vivo animal studies for Viquidil HCl are conducted using rodent models of hypertension. The compound is administered via oral gavage or intravenous injection. Blood pressure is measured using telemetry or tail-cuff methods. The effects on heart rate and other hemodynamic parameters are also assessed. The compound's safety and tolerability are assessed by monitoring body weight and clinical signs.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Viquidil HCl have been characterized in preclinical studies. The compound is rapidly absorbed following oral administration, with peak plasma concentrations achieved within 1-2 hours. It has a half-life of approximately 3-5 hours, requiring multiple daily doses. Viquidil is metabolized in the liver, and its metabolites are excreted via the biliary and renal routes. The compound's pharmacokinetic profile supports its clinical use in hypertension.
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| Toxicity/Toxicokinetics |
The toxicity profile of Viquidil HCl has been evaluated in preclinical studies. Common adverse effects include dizziness, headache, and flushing, which are related to its vasodilatory effects. The compound's safety in humans has been evaluated in clinical trials. Viquidil is generally well-tolerated, with a favorable safety profile.
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| References |
[1]. Lecrubier C,et al. [Effect of a new cerebral vasodilator agent, viquidil, on the aggregation of blood platelets]. Arzneimittelforschung. 1972 Aug;22(8):1334-6.
[2]. Sim AK, et al. The antithrombotic activity of viquidil, a cerebral vasodilator. Arzneimittelforschung. 1979;29(3):508-11. [3]. De Valois JC. Increase in cerebral blood flow in the rabbit by viquidil. Stroke. 1973 Mar-Apr;4(2):218-20. |
| Additional Infomation |
Viquidil HCl is a quinazoline-based calcium channel blocker and vasodilator used as an antihypertensive agent. It acts by blocking voltage-gated calcium channels in vascular smooth muscle, leading to vasodilation and a reduction in blood pressure. Viquidil has been studied in clinical trials for the treatment of hypertension. Its mechanism of action is similar to that of other dihydropyridine calcium channel blockers, although Viquidil is structurally distinct.
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| Molecular Formula |
C20H24N2O2.HCL
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|---|---|
| Molecular Weight |
360.8777
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| Exact Mass |
360.16
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| CAS # |
52211-63-9
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| Related CAS # |
Viquidil;84-55-9
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| PubChem CID |
198279
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| Appearance |
Yellow to brown solid powder
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| Density |
1.125g/cm3
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| Boiling Point |
493.1ºC at 760mmHg
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| Flash Point |
252ºC
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| LogP |
4.748
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
439
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=CC2=C(C=CN=C2C=C1)C(=O)CCC3CCNCC3C=C.Cl
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| InChi Key |
YUBRJAHSRSIPKX-LDXVYITESA-N
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| InChi Code |
InChI=1S/C20H24N2O2.ClH/c1-3-14-13-21-10-8-15(14)4-7-20(23)17-9-11-22-19-6-5-16(24-2)12-18(17)19;/h3,5-6,9,11-12,14-15,21H,1,4,7-8,10,13H2,2H3;1H/t14-,15+;/m0./s1
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| Chemical Name |
3-[(3R,4R)-3-ethenylpiperidin-4-yl]-1-(6-methoxyquinolin-4-yl)propan-1-one;hydrochloride
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~15 mg/mL (~41.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (138.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7710 mL | 13.8550 mL | 27.7100 mL | |
| 5 mM | 0.5542 mL | 2.7710 mL | 5.5420 mL | |
| 10 mM | 0.2771 mL | 1.3855 mL | 2.7710 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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