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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].
For research use only. We do not sell to patients.
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].
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.
Induction of chronic progressive pulmonary hypertension (PH)
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 Mmodeling Methods
Rat[10]: male • adult Sprague Dawley rats • 300-350 g Administration: 60 mg/kg • sc for 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 Record
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: Increased right ventricular systolic pressure, right heart hypertrophy, gas exchange; collagen deposition in the pulmonary artery.
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
ConcentrationSolventMass
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
10 mM
0.3074 mL
1.5368 mL
3.0735 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.
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.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
*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
ConcentrationSolventMass
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.
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.
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