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  5. Monocrotaline

Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].

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CAS No. : 315-22-0

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Based on 44 publication(s) in Google Scholar

Other Forms of Monocrotaline:

Monocrotaline Related Antibodies

Top Publications Citing Use of Products

44 Publications Citing Use of MCE Monocrotaline

WB
RT-PCR
IF
In Vivo Imaging
Histological Imaging/Staining

    Monocrotaline purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 7;10(1):3551.   [Abstract]

    CD146 protein expression in lungs with Monocrotaline (MCT, 50 mg/kg, i.p., 21 d)-induced PH in rats.

    Monocrotaline purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 7;10(1):3551.   [Abstract]

    CD146 mRNA expression in the lungs of rats during development of Monocrotaline (MCT, 50 mg/kg, i.p., 21 d)-induced PH.

    Monocrotaline purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 7;10(1):3551.   [Abstract]

    Representative immunofluorescence of CD146 (red) and αSMA (green) in small pulmonary arteries from rat lungs without or with Monocrotaline (MCT, 50 mg/kg, i.p., 21 d)-induced PH.

    Monocrotaline purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 7;10(1):3551.   [Abstract]

    Echocardiography measurements were carried out on anti-CD146- or mIgG-treated rats after 5 weeks of MCT (Monocrotaline, 50 mg/kg, i.p.) to determine PAAT, RVID, RVWT, TAPSE, CO, and CI (n = 10 rats per group).

    Monocrotaline purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 7;10(1):3551.   [Abstract]

    Representative images of H&E and immunofluorescent staining of PAs (20–50 μm or 51–100 μm in diameter) stained with αSMA (green). Monocrotaline treatment (MCT, 50 mg/kg, i.p., 21 d). Scale bar, 50 μm.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].
    IC50 & Target[8]

    OCT1

    36.8 μM (IC50)

    OCT2

    1852.6 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A204 IC50
    316 μg/mL
    Compound: 14
    Cytotoxicity against human A204 cells after 24 hrs by soft agar colony forming assay
    Cytotoxicity against human A204 cells after 24 hrs by soft agar colony forming assay
    		[PMID: 3210016]
    CHO EC50
    > 100 μg/mL
    Compound: 1
    Toxicity against Cricetulus griseus CHO (Chinese hamster ovary) cell by MTT assay
    Toxicity against Cricetulus griseus CHO (Chinese hamster ovary) cell by MTT assay
    		10.1016/jbse.2007.08.015
    KB ED50
    > 100 μg/mL
    Compound: Monocrotaline
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    		[PMID: 7130986]
    Sf9 EC50
    > 100 μg/mL
    Compound: 1
    Toxicity against Spodoptera frugiperda (fall armyworm) Sf9 cells by MTT assay
    Toxicity against Spodoptera frugiperda (fall armyworm) Sf9 cells by MTT assay
    		10.1016/jbse.2007.08.015
    In Vitro

    Monocrotaline a natural ligand exhibits dose-dependent cytotoxicity with potent antineoplastic activity. The in vitro cytotoxicity of monocrotaline is proved at IC50 24.966 μg/mL and genotoxicity at 2 X IC50 against HepG2 cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Monocrotaline Related Antibodies

    Cell Viability Assay[2]

    Cell Line: HepG2 cells
    Concentration: 25, 50, 100 and 200 µg/mL
    Incubation Time: 48 h
    Result: Induced apoptosis rate was dose-dependent.
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Monocrotaline can be used in animal modeling to construct a rat model of hypertension.

    MCT causes a pulmonary vascular syndrome in rats characterized by proliferative pulmonary vasculitis, pulmonary hypertension (PH), and cor pulmonale[3].
    Among preclinical models of pulmonary arterial hypertension (PAH), monocrotaline animal model offers the advantage of mimic several key aspects of human PAH, including vascular remodeling, proliferation of smooth muscle cells, endothelial dysfunction, upregulation of inflammatory cytokines, and right ventricle failure, requiring a single drug injection[4].
    Changes in multiple pathways associated with the development of PH, including activated glycolysis, increased markers of proliferation, disruptions in carnitine homeostasis, increased inflammatory and fibrosis biomarkers, and a reduction in glutathione biosynthesis are observed with the injection of monocrotaline[5].
    Monocrotaline (60 mg/kg; i.p.; single dose), followed by Astragaloside (ASIV) (10 and 30 mg/kg/day for 21 days), significantly increases pulmonary artery pressure and promotes pulmonary artery structural remodeling and right ventricular hypertrophy in rats[7].
    Monocrotaline (60 mg/kg; i.p.; single dose) causes Pulmonary arterial hypertension (PAH) in rat models in 3-4 weeks[7].
    Monocrotaline (60 mg/kg; i.p. Single dose), 7 days after surgery, exhibits dose-dependent cytotoxicity and shows potent antitumor activity in a rat model of left pneumonectomy [9].
    NOTE: Monocrotaline is dissolved in 1 N HCl, diluted in sterile saline and adjusted to pH 7.0 with 1 N NaOH[7].
    Induction of Chronic Progressive Pulmonary Hypertension (PH)[10][11]
    Background
    Pulmonary arterial hypertension (PAH) is characterized by vascular remodeling of the distal pulmonary arterial circulation. PAH remodeling includes apoptosis and proliferation of pulmonary vascular endothelial cells, muscularization of distal pulmonary arterioles, deposition of extracellular matrix proteins, and perivascular inflammation; it is accompanied by increased pulmonary vascular resistance, leading to right ventricular (RV) failure and death. However, the cause of pulmonary vascular remodeling in PAH is still unclear. Monocrotaline induces right ventricular hypertrophy (RVH) and pulmonary vascular remodeling.
    Specific Modeling Methods
    Rat[10]: male • adult Sprague Dawley rats • 300-350 g
    Administration: 60 mg/kg • sc • single dose • Control group: saline solution
    Mcie[11]: male ? C57BL/6 mice • 6-8 weeks old
    Administration: 600 mg/kg • sc • once weekly for 4 weeks
    Note
    (1) Monocrotaline-induced pulmonary hypertension can be reversed by tail vein injection of 25 μg mouse mesenchymal stem cells in 100 μL PBS three hours after each injection.
    (2) Extracellular vesicles (EVs) isolated from the circulation or lungs of mice with monocrotaline-induced pulmonary hypertension induce right ventricular hypertrophy (RVH) and pulmonary vascular remodeling when injected into healthy mice.
    Modeling Indicators
    Molecular changes: Expression of 5-HTR2A, 5-HTR2B and 5-HTT in lung homogenate ↑ ; expression of IL-1b, IL6, TNF-a and MCP-1 ↑; levels of total collagen fibers and total pulmonary vascular collagen ↑.
    Physiological indicators: Right ventricular systolic pressure ↑; right heart hypertrophy, gas exchange; collagen deposition in the pulmonary artery ↑.
    Correlated Product(s): Terguride (HY-12714)

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    325.36

    Formula

    C16H23NO6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O[C@]1([H])CCN2[C@]1([H])C(CO3)=CC2)[C@H](C)[C@@](C)(O)[C@@](C)(O)C3=O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    1M HCl : 100 mg/mL (307.35 mM; adjust pH to 1 with HCl)

    DMSO : 25 mg/mL (76.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 2 mg/mL (6.15 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0735 mL 15.3676 mL 30.7352 mL
    5 mM 0.6147 mL 3.0735 mL 6.1470 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (7.68 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.68 mM); Suspended solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 4.17 mg/mL (12.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    • Protocol 2

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 21 mg/mL (64.54 mM); Clear solution; Need ultrasonic and warming and heat to 53°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    SDS (644 KB)

    COA (260 KB) HNMR (234 KB) RP-HPLC (266 KB) MS (185 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO / 1M HCl 1 mM 3.0735 mL 15.3676 mL 30.7352 mL 76.8380 mL
    5 mM 0.6147 mL 3.0735 mL 6.1470 mL 15.3676 mL
    DMSO / 1M HCl 10 mM 0.3074 mL 1.5368 mL 3.0735 mL 7.6838 mL
    15 mM 0.2049 mL 1.0245 mL 2.0490 mL 5.1225 mL
    20 mM 0.1537 mL 0.7684 mL 1.5368 mL 3.8419 mL
    25 mM 0.1229 mL 0.6147 mL 1.2294 mL 3.0735 mL
    30 mM 0.1025 mL 0.5123 mL 1.0245 mL 2.5613 mL
    40 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9209 mL
    50 mM 0.0615 mL 0.3074 mL 0.6147 mL 1.5368 mL
    60 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2806 mL
    1M HCl 80 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9605 mL
    100 mM 0.0307 mL 0.1537 mL 0.3074 mL 0.7684 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Monocrotaline Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Monocrotaline315-22-0CrotalineOthersOCT-1OCT-2antitumor activitycytotoxicity of cellsPulmonary arterial hypertension modelInhibitorinhibitorinhibit

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