| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
- Catharanthine Tartrate (referred to as "Catharanthine" in literature) inhibits voltage-operated calcium channels (VOCC) in vascular smooth muscle cells and cardiomyocytes[1]
- Catharanthine Tartrate (specifically (+)-Catharanthine) acts on serotonergic and norepinephrinergic neurotransmission systems to exert antidepressant-like effects (targets: 5-hydroxytryptamine receptors, α2-adrenergic receptors)[2] |
|---|---|
| ln Vitro |
- Vasodilatory effect on isolated mesenteric arteries: Isolated rat small mesenteric artery rings were pre-contracted with KCl (60 mM). Treatment with Catharanthine Tartrate (10, 30, 100 μM) induced concentration-dependent relaxation. At 100 μM, the relaxation rate was 65% compared to the pre-contracted state. This effect was reversed by increasing extracellular Ca²⁺ concentration (from 1.8 mM to 5 mM), confirming VOCC inhibition as the mechanism[1]
- Inhibition of cardiomyocyte calcium currents: In whole-cell patch-clamp experiments on isolated rat ventricular myocytes, Catharanthine Tartrate (10, 30, 100 μM) inhibited VOCC-mediated Ca²⁺ currents. At 100 μM, the current amplitude was reduced by 58% compared to the control group (no drug treatment). The inhibition was voltage-independent, affecting both L-type and T-type VOCCs[1] |
| ln Vivo |
- Cardiovascular effects in rats: Male Wistar rats (280-320 g) were anesthetized, and arterial catheters were implanted to monitor heart rate (HR), systolic blood pressure (SBP), and left ventricular contractility (dP/dt max). Intravenous administration of Catharanthine Tartrate (1, 3, 10 mg/kg) caused dose-dependent decreases: 10 mg/kg reduced HR by 28%, SBP by 22%, and dP/dt max by 30% compared to the baseline. The effects peaked at 5 minutes post-administration and lasted for 20-30 minutes[1]
- Antidepressant-like activity in mice: Male ICR mice (20-25 g) were treated with intraperitoneal injection of (+)-Catharanthine Tartrate (10, 20 mg/kg). Thirty minutes later, the forced swim test (FST) and tail suspension test (TST) were performed. In FST, 20 mg/kg reduced immobility time by 45% compared to the control (saline-injected); in TST, it reduced immobility time by 40%. Pretreatment with the 5-HT1A receptor antagonist WAY-100635 (1 mg/kg, i.p.) or the α2-adrenergic receptor antagonist yohimbine (1 mg/kg, i.p.) completely reversed these effects[2] |
| Cell Assay |
- Cardiomyocyte VOCC current recording: Rat ventricular myocytes were isolated via collagenase perfusion and maintained in oxygenated Tyrode’s solution. Whole-cell patch-clamp configuration was established with a glass pipette filled with intracellular solution (containing CsCl to block K⁺ currents). Catharanthine Tartrate (10, 30, 100 μM) was added to the extracellular solution, and Ca²⁺ currents were recorded at holding potentials of -80 mV, with step depolarizations to -40 mV to +60 mV. Current amplitude and kinetics were analyzed using electrophysiology software to quantify inhibition[1]
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| Animal Protocol |
- Rat cardiovascular function assay: Male Wistar rats (280-320 g) were anesthetized with an intraperitoneal injection of anesthetic. A polyethylene catheter was inserted into the femoral artery to measure SBP and HR via a pressure transducer, and another catheter was inserted into the left ventricle via the right carotid artery to record dP/dt max (index of contractility). After 30 minutes of stabilization, Catharanthine Tartrate (dissolved in normal saline, 1, 3, 10 mg/kg) was administered intravenously via the femoral vein. Hemodynamic parameters were recorded continuously for 60 minutes post-administration[1]
- Mouse antidepressant behavioral assays: Male ICR mice (20-25 g) were randomly divided into 4 groups (n=8/group): control (saline, i.p.), (+)-Catharanthine Tartrate 10 mg/kg (i.p.), (+)-Catharanthine Tartrate 20 mg/kg (i.p.), and antagonist-pretreated group (WAY-100635 or yohimbine 1 mg/kg, i.p., 15 minutes before (+)-Catharanthine Tartrate 20 mg/kg). For FST: mice were placed in a water-filled cylinder (25°C, 15 cm depth) for 6 minutes, and immobility time was recorded during the last 4 minutes. For TST: mice were suspended by the tail (15 cm above the floor) for 6 minutes, and immobility time was recorded during the last 4 minutes[2] |
| References |
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| Additional Infomation |
Vincristine tartrate is a monoterpenoid indole alkaloid isolated from plants of the genus Catharanthus (e.g., Catharanthus vinca) [1,2]
- Vincristine tartrate exhibits vasomotor and cardiac depressive effects mediated by inhibition of voltage-gated calcium channels (VOCC), thereby reducing Ca²⁺ inflow into vascular smooth muscle cells (relaxation) and cardiomyocytes (reduced contractility and heart rate) [1] - Vincristine tartrate exhibits subtype-specific antidepressant-like activity (only the (+)-enantiomer is active) and depends on activation of serotonergic (5-HT1A receptor dependent) and noradrenergic (α2-adrenergic receptor dependent) neurotransmission [2] |
| Molecular Formula |
C21H24N2O2.C4H6O6
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|---|---|
| Molecular Weight |
486.5143
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| Exact Mass |
822.383
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| CAS # |
4168-17-6
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| Related CAS # |
Catharanthine;2468-21-5;Catharanthine Sulfate;153230-94-5
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| PubChem CID |
24721367
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| Appearance |
Off-white to gray solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
737
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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.C(C(C(=O)O)O)(C(=O)O)O
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| InChi Key |
JYBKPXVXYJDIFX-GYMDHWDQSA-N
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| InChi Code |
InChI=1S/C21H24N2O2.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h4-7,10,13,19,22H,3,8-9,11-12H2,1-2H3;1-2,5-6H,(H,7,8)(H,9,10)/t13-,19+,21-;/m0./s1
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| Chemical Name |
2,3-dihydroxybutanedioic acid;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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~205.55 mM)
H2O : ~5 mg/mL (~10.28 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 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 25.0 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: ≥ 2.5 mg/mL (5.14 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 25.0 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: ≥ 2.5 mg/mL (5.14 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 | 2.0555 mL | 10.2773 mL | 20.5546 mL | |
| 5 mM | 0.4111 mL | 2.0555 mL | 4.1109 mL | |
| 10 mM | 0.2055 mL | 1.0277 mL | 2.0555 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.