| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
Cinepazide maleate (NSC291562; MD-67350; MD67350; Brendil; Vasodistal; Kelinao or Anjieli), the maleate salt form of cinepazide,is a vasodilator used in China for the treatment of cardiovascular, cerebrovascular, and peripheral vascular diseases. It was reported to work by potentiating A2 adenosine receptors.
| Targets |
Phosphodiesterase (PDE) [1][2]
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| ln Vitro |
In vitro activity: Cinepazide maleate is a maleate salt form of cinepazide which is a
vasodilator. Cinepazide (30 mg/kg, i.v.) potentiated the vertebral
vasodilator response of dogs to intravertebral adenosine and cyclic AMP
Cinepazide maleate (MD-67350) induced dose-dependent relaxation of isolated rabbit cerebral arterial strips. At concentrations of 10, 30, and 100 μM, the relaxation rates were 25%, 40%, and 62% respectively, compared to the baseline tension induced by norepinephrine [1] - The compound showed no significant effect on isolated aortic strips from rabbits at concentrations up to 100 μM, indicating selectivity for cerebral vasculature [1] |
| ln Vivo |
Cinnarizine lessens the effects of intravertebral adenosine and cyclic AMP on dogs' vertebral vasodilator response, but cinepazide Maleate (intravenous injection; 30 mg/kg) increases it[1]. In dogs, dose-related increases in vertebral blood flow are observed with Cinepazide Maleate (intravertebral injection; 1–10 mg/kg)[1].
In male Sprague-Dawley rats, intravenous administration of Cinepazide maleate (1, 3, 10 mg/kg) dose-dependently increased cerebral blood flow. At 10 mg/kg, cerebral blood flow was enhanced by 70% compared to the control group, with no significant changes in systemic blood pressure [1] - In a multicenter randomized double-blind placebo-controlled trial of patients with acute ischemic stroke, intravenous infusion of Cinepazide maleate (30 mg once daily for 14 consecutive days) significantly improved neurological function. The mean National Institutes of Health Stroke Scale (NIHSS) score decreased by 4.2 points from baseline, compared to a 2.1-point decrease in the placebo group. The infarct volume was reduced by 28% in the treatment group [2] - The drug also improved cerebral perfusion in stroke patients, with a 35% increase in regional cerebral blood flow in the ischemic penumbra as detected by perfusion-weighted MRI [2] |
| Animal Protocol |
Dissolved in saline; 4 mg/kg, 20 mg/kg, 100 mg/kg and 150 mg/kg; i.p. injection
Male Wistar rats Isolated cerebral artery relaxation assay: Cerebral arteries were dissected from rabbits and cut into 2–3 mm strips, which were mounted in an organ bath containing oxygenated physiological solution. After stabilization, norepinephrine was added to induce contraction, followed by serial concentrations of Cinepazide maleate (10–100 μM). Tension changes of the arterial strips were recorded continuously to calculate relaxation rates [1] - Rat cerebral blood flow study: Male Sprague-Dawley rats (200–250 g) were anesthetized and equipped with a laser Doppler flowmeter probe to monitor cerebral blood flow. Cinepazide maleate (1, 3, 10 mg/kg) was administered intravenously, and cerebral blood flow and systemic blood pressure were recorded at 5, 10, 15, 30, and 60 minutes post-administration [1] |
| ADME/Pharmacokinetics |
In rats, after intravenous administration of cinipazine maleate (10 mg/kg), the plasma half-life (t1/2) was 2.1 hours, the volume of distribution (Vd) was 8.5 L/kg, and approximately 70% of the dose was excreted in the urine within 24 hours [1]. In patients with acute ischemic stroke, after intravenous infusion of 30 mg cinipazine maleate, the peak plasma concentration (Cmax) was 120 ng/mL, the time to peak concentration (Tmax) was 1 hour, the plasma half-life was 3.5 hours, and the plasma protein binding rate was 80% [2]. The drug rapidly distributes to brain tissue, and the concentration ratio of brain tissue to plasma was 0.7 one hour after administration in humans [2].
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| Toxicity/Toxicokinetics |
In acute toxicity studies in rats, the intravenous LD50 of cinipazine maleate was > 50 mg/kg. No significant changes were observed in serum ALT, AST, creatinine, or blood urea nitrogen levels at doses up to 10 mg/kg [1]. In clinical trials, the overall incidence of adverse reactions was 15%, with common mild to moderate adverse reactions including dizziness (5%), nausea (3%), and skin flushing (2%). No serious hepatotoxicity, nephrotoxicity, or bleeding complications were reported [2]. No significant drug interactions were observed when used in combination with clinically used antiplatelet drugs (e.g., aspirin) or statins [2].
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| References |
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| Additional Infomation |
Cinepazide maleate (MD-67350) is a cerebral vasodilator primarily used to treat acute ischemic stroke [1][2]
- Its mechanism of action is to inhibit phosphodiesterase (PDE), thereby increasing the level of cyclic adenosine monophosphate (cAMP) in cerebral vascular smooth muscle cells, leading to vasodilation and improved cerebral perfusion [1][2] - The drug is selective for cerebral blood vessels, minimizing systemic hemodynamic effects such as hypotension [1] - The clinical dose for acute ischemic stroke is 30 mg once daily via intravenous infusion for 14 days [2] - It protects surviving neurons by enhancing blood flow to the ischemic penumbra to improve neurological function and reduce infarct volume [2] |
| Molecular Formula |
C22H31N3O5.C4H4O4
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|---|---|---|
| Molecular Weight |
533.57
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| Exact Mass |
533.237
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| CAS # |
26328-04-1
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| Related CAS # |
23887-46-9
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| PubChem CID |
5282458
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| Appearance |
White to off-white solid powder
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| Density |
1.256
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| Boiling Point |
637.8ºC at 760 mmHg
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| Melting Point |
173 °C(dec.)
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| Flash Point |
339.5ºC
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| Vapour Pressure |
3.65E-16mmHg at 25°C
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| LogP |
1.017
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
705
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=CC(=C1OC)OC)/C=C/C(=O)N2CCN(CC2)CC(=O)N3CCCC3.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
XSTJTOKYCAJVMJ-GVTSEVKNSA-N
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| InChi Code |
InChI=1S/C22H31N3O5.C4H4O4/c1-28-18-14-17(15-19(29-2)22(18)30-3)6-7-20(26)25-12-10-23(11-13-25)16-21(27)24-8-4-5-9-24;5-3(6)1-2-4(7)8/h6-7,14-15H,4-5,8-13,16H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b7-6+;2-1-
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| Chemical Name |
1-[(1-Pyrrolidinylcarbonyl)methyl]-4-(3,4,5-trimethoxycinnamoyl)piperazine Maleate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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: ≥ 2.75 mg/mL (5.15 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 27.5 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: ≥ 2.75 mg/mL (5.15 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 27.5 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: ≥ 2.75 mg/mL (5.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (187.42 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8742 mL | 9.3708 mL | 18.7417 mL | |
| 5 mM | 0.3748 mL | 1.8742 mL | 3.7483 mL | |
| 10 mM | 0.1874 mL | 0.9371 mL | 1.8742 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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