| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Calcium channels in vascular smooth muscle cells. Cadralazine acts as a peripheral arteriolar vasodilator by inhibiting calcium ion influx into smooth muscle cells, leading to vasodilation, improved blood flow, decreased vascular resistance, and reduced blood pressure. The compound is an orally bioactive antihypertensive agent.
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|---|---|
| ln Vitro |
Cadralazine acts as a peripheral arteriolar vasodilator by inhibiting calcium ion influx into smooth muscle cells. This leads to vasodilation, improved blood flow, decreased vascular resistance, and reduced blood pressure. The compound is reportedly better-tolerated and longer-acting than hydralazine and is useful as a second-line treatment in hypertension.
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| ln Vivo |
Cadralazine is an orally bioactive antihypertensive agent used for the treatment of hypertension. It acts as a peripheral arteriolar vasodilator by inhibiting calcium influx into smooth muscle cells, leading to decreased vascular resistance and reduced blood pressure. The compound is reportedly better-tolerated and longer-acting than hydralazine.
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| Enzyme Assay |
In vitro assays for cadralazine involve measuring its effects on vascular smooth muscle contraction and calcium influx. Isolated vascular smooth muscle preparations are treated with cadralazine, and contraction is measured in response to vasoconstrictors. The compound's ability to inhibit calcium influx is assessed using fluorescent calcium indicators or patch-clamp electrophysiology.
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| Cell Assay |
In vitro cellular assays for cadralazine involve treating vascular smooth muscle cells with the compound and measuring calcium influx, cell contraction, or proliferation. Cells are loaded with calcium-sensitive fluorescent dyes and treated with cadralazine. Changes in intracellular calcium concentration are measured. The compound inhibits calcium ion influx into smooth muscle cells.
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| Animal Protocol |
In vivo animal studies for cadralazine typically involve administration to hypertensive animal models to assess its antihypertensive effects. Blood pressure is measured via telemetry or tail-cuff plethysmography. Cadralazine acts as a peripheral arteriolar vasodilator, decreasing vascular resistance and reducing blood pressure.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of cadralazine show that the compound is orally bioactive. It has a molecular weight of 283.33 and a molecular formula of C12H21N5O3. The compound has a melting point of 160-162°C and a pKa of 6.0. UV maximum absorption is at 248 and 340 nm. Cadralazine is classified as an active pharmaceutical ingredient.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of cadralazine have established its safety profile for use as an antihypertensive agent. The compound is reportedly better-tolerated than hydralazine. Common adverse effects may include headache, flushing, and palpitations due to its vasodilatory action. The compound should be used under medical supervision.
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| Additional Infomation |
Cadralazine is an organic molecular entity.
Cadralazine (ISF 2469) is a hydrazinophthalazine-derivative antihypertensive agent classified as a peripheral arteriolar vasodilator. It acts by inhibiting calcium ion influx into smooth muscle cells, leading to vasodilation, decreased vascular resistance, and reduced blood pressure. The compound is orally bioactive and is reportedly better-tolerated and longer-acting than hydralazine. It is useful as a second-line treatment in the management of hypertension. |
| Molecular Formula |
C12H21N5O3
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|---|---|
| Molecular Weight |
283.33
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| Exact Mass |
283.164
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| CAS # |
64241-34-5
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| PubChem CID |
2515
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| Appearance |
White to off-white solid powder
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| Density |
1.253 g/cm3
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| Boiling Point |
425.88°C (rough estimate)
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| Melting Point |
160-162°
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| Index of Refraction |
1.59
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| LogP |
1.22
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
20
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| Complexity |
292
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(O)CN(C1=NN=C(NNC(OCC)=O)C=C1)CC
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| InChi Key |
QLTVVOATEHFXLT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H21N5O3/c1-4-17(8-9(3)18)11-7-6-10(13-15-11)14-16-12(19)20-5-2/h6-7,9,18H,4-5,8H2,1-3H3,(H,13,14)(H,16,19)
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| Chemical Name |
ethyl N-[[6-[ethyl(2-hydroxypropyl)amino]pyridazin-3-yl]amino]carbamate
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| Synonyms |
ISF 2469; ISF-2469; Cadralazine
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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 (~882.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.34 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 (7.34 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 (7.34 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 | 3.5295 mL | 17.6473 mL | 35.2945 mL | |
| 5 mM | 0.7059 mL | 3.5295 mL | 7.0589 mL | |
| 10 mM | 0.3529 mL | 1.7647 mL | 3.5295 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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