An antagonist of neuronal nicotinic AChRs
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MG624

Item No. 24298

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N,N-triethyl-2-[4-[(1E)-2-phenylethenyl]phenoxy]-ethanaminium, monoiodide
CAS Number
77257-42-2
Molecular Formula
C22H30NO • I
Formula Weight
451.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mMPBS (pH 7.2): 0.3 mg/ml
λmax
204, 224, 302 nm
SMILES
CC[N+](CC)(CC)CCOC(C=C1)=CC=C1/C=C/C2=CC=CC=C2.[I-]
InChi Code
InChI=1S/C22H30NO.HI/c1-4-23(5-2,6-3)18-19-24-22-16-14-21(15-17-22)13-12-20-10-8-7-9-11-20;/h7-17H,4-6,18-19H2,1-3H3;1H/q+1;/p-1/b13-12+;
InChi Key
RDTKUZXIHMTSJO-UEIGIMKUSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $169

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    Product Description

    MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 0.055 µM in neuronal chick optic lobe membranes).1 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).2 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).3 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gotti, C., Balestra, B., Morretti, M., et al. 4-Oxystilbene compounds are selective ligands for neuronal nicotinic αBungarotoxin receptors. Br. J. Pharmacol. 124(6), 1197-1206 (1998).

    2. Vailati, S., Moretti, M., Longhi, R., et al. Developmental expression of heteromeric nicotinic receptor subtypes in chick retina. Mol. Pharmacol. 63(6), 1329-1337 (2003).

    3. Brown, K.C., Lau, J.K., Dom, A.M., et al. MG624, an α7-nAChR antagonist, inhibits angiogenesis via the Egr-1/FGF2 pathway. Angiogenesis 15(1), 99-114 (2012).