An antagonist of neuronal nicotinic AChRs (Ki = 0.055 µM); selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM); inhibits acetylcholine-evoked currents in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 95 nM); selective for α7 subunit-containing nAChRs over α6

MG624 – 10 mg

Brand:
Cayman
CAS:
77257-42-2
Storage:
-20
UN-No:
Non-Hazardous - /

MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 0.055 µM in neuronal chick optic lobe membranes).{42205} It is selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM in TE671 cells that express muscle-type AChRs). MG624 inhibits currents evoked by acetylcholine in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 94 nM). It is selective for α7 subunit-containing nAChRs over α6, β2, and β4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively).{42206} It selectively decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM) over isolated rat phrenic nerve-hemidiaphragm preparations (EC50 = 486 µM). MG624 decreases protein levels of early growth response gene 1 (Egr-1) induced by nicotine in human microvascular endothelial cells of the lung (HMEC-Ls).{42207} It also decreases proliferation of HMEC-Ls and inhibits angiogenesis in vitro and ex vivo as well as in an H69 small cell lung cancer (SCLC) mouse xenograft model concomitant with a reduction in tumor growth when administered in the diet at a dose of approximately 10 mg/kg per day.  

 

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Description

An antagonist of neuronal nicotinic AChRs (Ki = 0.055 µM); selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM); inhibits acetylcholine-evoked currents in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 95 nM); selective for α7 subunit-containing nAChRs over α6, β2, and β4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively); decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM); decreases Egr-1 protein levels in and proliferation of HMEC-Ls; decreases angiogenesis in vitro, ex vivo, and in an H69 SCLC mouse xenograft model at approximately 10 mg/kg per day as well as reduces tumor growth in the H69 SCLC mouse xenograft model

Formal name: N,N,N-triethyl-2-[4-[(1E)-2-phenylethenyl]phenoxy]-ethanaminium, monoiodide

Synonyms: 

Molecular weight: 451.4

CAS: 77257-42-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cancer|Angiogenesis||Research Area|Neuroscience

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