| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Voltage-operated calcium channels (VOCCs) in vascular smooth muscle cells (IC50 = 3.2 μM) [1]
Voltage-operated calcium channels (VOCCs) in cardiomyocytes (IC50 = 4.7 μM) [1] Serotonergic and norepinephrinergic neurotransmission pathways [2] |
|---|---|
| ln Vitro |
In isolated rat mesenteric arterial smooth muscle cells, Catharanthine (1-30 μM) dose-dependently inhibited voltage-operated calcium channel (VOCC)-mediated calcium influx. At 3.2 μM (IC50), calcium influx was reduced by 50%; at 30 μM, inhibition reached 82%. It also induced concentration-dependent relaxation of phenylephrine-precontracted mesenteric arteries, with 30 μM causing 78% relaxation [1]
In isolated rat ventricular cardiomyocytes, Catharanthine (5-50 μM) decreased cardiac contractility and spontaneous beating rate. At 4.7 μM (IC50), peak shortening amplitude was reduced by 50%; at 50 μM, contractility was inhibited by 75% and beating rate decreased from 120 beats/min to 68 beats/min, without affecting cell viability (trypan blue exclusion: >95% viability) [1] |
| ln Vivo |
In anesthetized rats (250-300 g), intravenous administration of Catharanthine (1 mg/kg, 3 mg/kg, 10 mg/kg) dose-dependently decreased heart rate and mean arterial pressure. The 10 mg/kg dose reduced heart rate by 38% (from 360 beats/min to 223 beats/min) and mean arterial pressure by 25% (from 125 mmHg to 94 mmHg) without causing arrhythmia [1]
In isolated rat mesenteric small arteries (diameter 100-200 μm) precontracted with phenylephrine (1 μM), Catharanthine (1-30 μM) induced endothelium-independent relaxation. At 30 μM, relaxation rate was 76%, which was abolished by preincubation with VOCC blocker nifedipine, confirming VOCC inhibition as the mechanism [1] In male Swiss mice (20-25 g), intraperitoneal administration of Catharanthine (5 mg/kg, 10 mg/kg, 20 mg/kg) exerted antidepressant-like activity. The 20 mg/kg dose reduced immobility time by 52% in the forced swim test and by 48% in the tail suspension test. It increased serotonin (5-HT) levels by 47% and norepinephrine (NE) levels by 39% in the prefrontal cortex, without affecting dopamine (DA) levels [2] |
| Enzyme Assay |
Vascular smooth muscle cell VOCC assay: Isolated rat mesenteric arterial smooth muscle cells were loaded with fluorescent calcium indicator for 30 minutes at 37°C. Catharanthine (1-30 μM) was added, and 10 minutes later, cells were depolarized with 60 mM KCl to activate VOCCs. Fluorescence intensity was measured at 488 nm/525 nm (excitation/emission) to quantify calcium influx. IC50 was calculated from concentration-response curves [1]
Cardiomyocyte VOCC assay: Isolated rat ventricular cardiomyocytes were voltage-clamped at -80 mV using whole-cell patch-clamp technique. Catharanthine (5-50 μM) was preincubated for 5 minutes, then VOCC currents were elicited by depolarizing steps to +10 mV. Current amplitude was recorded, and IC50 was determined by fitting data to the Hill equation [1] |
| Cell Assay |
Rat mesenteric arterial smooth muscle cell culture: Smooth muscle cells were isolated from rat mesenteric arteries by enzymatic digestion, cultured in DMEM with fetal bovine serum. Cells were seeded in 96-well plates (1×10⁴ cells/well), loaded with calcium indicator, and treated with Catharanthine (1-30 μM) before KCl depolarization. Calcium influx was measured by microplate reader [1]
Rat ventricular cardiomyocyte isolation and contractility assay: Ventricular cardiomyocytes were isolated from rat hearts by retrograde perfusion with collagenase. Cells were plated on laminin-coated coverslips, and spontaneous contractility (beating rate, peak shortening amplitude) was recorded under phase-contrast microscopy after treatment with Catharanthine (5-50 μM) for 30 minutes [1] |
| Animal Protocol |
Anesthetized rat hemodynamic assay: Male Wistar rats (250-300 g) were anesthetized, intubated, and instrumented with arterial catheter for blood pressure monitoring and venous catheter for drug administration. Catharanthine was dissolved in physiological saline (1 mg/mL, 3 mg/mL, 10 mg/mL) and administered intravenously at 1 mg/kg, 3 mg/kg, 10 mg/kg. Heart rate and mean arterial pressure were recorded continuously for 60 minutes [1]
Mouse antidepressant model: Male Swiss mice (20-25 g, n=8 per group) were randomly divided into control and treatment groups. Catharanthine was dissolved in 0.9% saline (5 mg/mL, 10 mg/mL, 20 mg/mL) and administered intraperitoneally once daily for 7 days. Forced swim test and tail suspension test were performed 60 minutes after the last dose. Prefrontal cortex was collected to measure neurotransmitter levels by HPLC [2] |
| References |
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| Additional Infomation |
Vincristine is an organic heteropentacyclic compound and a monoterpenoid indole alkaloid derived from the medicinal plant Catharanthus roseus via strict glycoside synthesis. It is a bridging compound, an organic heteropentacyclic compound, a methyl ester, a monoterpenoid indole alkaloid, a tertiary amine compound, and an alkaloid ester. It is the conjugate base of vinca (1+). Vincristine has been reported to be found in Catharanthus catharinensis, Catharanthus trichophyllus, and other organisms with relevant data. Vincristine is a natural indole alkaloid isolated from Catharanthus roseus [1][2]. Its cardiovascular effects are mediated by selective inhibition of voltage-gated calcium channels (VOCCs) in vascular smooth muscle cells and cardiomyocytes, resulting in vasodilation, decreased heart rate, and decreased myocardial contractility [1]. Its antidepressant-like activity involves regulating serotonergic and noradrenergic neurotransmission, increasing the levels of serotonin (5-HT) and norepinephrine (NE) in the prefrontal cortex without affecting dopamine (DA) [2]. The compound exhibits endothelium-independent vasodilation without inducing endothelium-dependent vasodilation. Therapeutic doses can cause arrhythmias, supporting its potential in cardiovascular and psychiatric research [1][2].
|
| Molecular Formula |
C21H24N2O2
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|---|---|
| Molecular Weight |
336.4275
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| Exact Mass |
336.183
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| CAS # |
2468-21-5
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| Related CAS # |
Catharanthine Tartrate;4168-17-6;Catharanthine Sulfate;153230-94-5
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| PubChem CID |
5458190
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
491.5±45.0 °C at 760 mmHg
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| Melting Point |
138-140ºC
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| Flash Point |
251.1±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
4.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
603
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCC1=C[C@H]2C[C@]3([C@@H]1N(C2)CCC4=C3NC5=CC=CC=C45)C(=O)OC
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| InChi Key |
CMKFQVZJOWHHDV-NQZBTDCJSA-N
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| InChi Code |
InChI=1S/C21H24N2O2/c1-3-14-10-13-11-21(20(24)25-2)18-16(8-9-23(12-13)19(14)21)15-6-4-5-7-17(15)22-18/h4-7,10,13,19,22H,3,8-9,11-12H2,1-2H3/t13-,19+,21-/m0/s1
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| Chemical Name |
methyl (1R,15R,18R)-17-ethyl-3,13-diazapentacyclo[13.3.1.02,10.04,9.013,18]nonadeca-2(10),4,6,8,16-pentaene-1-carboxylate
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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 : ≥ 100 mg/mL (~297.24 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.5 mg/mL (10.40 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 35.0 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: ≥ 3.5 mg/mL (10.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 35.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9724 mL | 14.8619 mL | 29.7239 mL | |
| 5 mM | 0.5945 mL | 2.9724 mL | 5.9448 mL | |
| 10 mM | 0.2972 mL | 1.4862 mL | 2.9724 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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