Product Name
Monocrotaline
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.
Structural Formula
Monocrotaline
Solubility
1M HCl : 200 mg/mL(614.70 mM;Need ultrasonic) DMSO : 25 mg/mL(76.84 mM;ultrasonic and warming and heat to 60°C) H2O : 2 mg/mL(6.15 mM;Need ultrasonic)
Source
Plants >Leguminosae > Crotalaria pallidaAit.
Storage
4℃, sealed storage, away from moisture and light
Shipping
Room temperature in continental US; may vary elsewhere.
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
In Vivo
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. 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. 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.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.Monocrotaline (60 mg/kg; i.p.; single dose) causes Pulmonary arterial hypertension (PAH) in rat models in 3-4 weeks.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 7.4 with 1 N NaOH.
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.
Datasheet 
