Formulation: A solid
Formal Name: (αE,2S,3R,12bR)-3-ethyl-1,2,3,4,6,7,12,12b-octahydro-α-(methoxymethylene)-indolo[2,3-a]quinolizine-2-acetic acid, methyl ester
Purity: ≥98%
Formula Markup: C22H28N2O3
Formula Weight: 368,5
Shelf life (days): 730
CAS Number: 7729-23-9
Notes: Hirsutine is an indole that has been found in U. rhynchophylla and has diverse biological activities.{65701,65702,65703,65704} It selectively inhibits butyrylcholinesterase (BChE; IC50s = 1.97 and 4.97 µM for the human and horse enzymes, respectively) over eel acetylcholinesterase, for which it has no activity.{65703} Hirsutine also inhibits the homomeric serotonin (5-HT) receptor subtype 5-HT3A and heteromeric 5-HT3 receptors containing both A and B subunits (IC50s = 65.35 and 28.44 µM, respectively).{65704} It reduces glutamate-induced increases in cell death in HT22 cells when used at concentrations of 50 and 100 µM.{65701} Hirsutine (40, 60, and 80 µM) induces apoptosis in A549 and H1299 human non-small cell lung cancer (NSCLC) cells.{65702} It also reduces levels of Rho-associated kinase 1 (ROCK1) and phosphorylated glycogen synthase kinase 3β (GSK3β), as well as increases the level of phosphorylated phosphatase and tensin homolog (PTEN), in A549 cells.{65702} Hirsutine (10 mg/kg) reduces tumor growth and intratumoral levels of phosphorylated GSK3β in an A549 mouse xenograft model. It also reduces infarct size and cardiac cell apoptosis and prevents cardiac dysfunction in a rat model of ischemia-reperfusion injury when administered at a dose of 20 mg/kg.{65704}
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