Synonym
MG624; MG 624; MG-624
IUPAC/Chemical Name
N,N,N-triethyl-2-[4-[(1E)-2-phenylethenyl]phenoxy]-ethanaminium, monoiodide
InChi Key
RDTKUZXIHMTSJO-UEIGIMKUSA-M
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+;
SMILES Code
CC[N+](CC)(CC)CCOC1=CC=C(/C=C/C2=CC=CC=C2)C=C1.[I-]
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM.
In vitro activity:
MG624 (100 nm) reduced IACh peak amplitude by 59.7% at 100 μm ACh without affecting current decay (T0.1=0.13±0.03 s). The inhibition of IACh by MG624 was dose-dependent; the IC50 was 109 nm (Figure 4A, lower part) and remained similar when the Ca2+ was substituted by an equimolar concentration of Ba2+ (three oocytes, data not shown).
Reference: Br J Pharmacol. 1999 Jan;126(1):285-95. https://pubmed.ncbi.nlm.nih.gov/10051147/
In vivo activity:
The anti-angiogenic activity of MG624 was assessed by two in vivo models, namely the chicken chorioallantoic membrane model and the nude mice model. In both of these experimental models, MG624 inhibited angiogenesis of human SCLC tumors. Most importantly, the administration of MG624 was not associated with any toxic side effects, lethargy or discomfort in the mice. The anti-angiogenic activity of MG624 was mediated via the suppression of nicotine-induced FGF2 levels in HMEC-Ls. MG624 decreased nicotine-induced early growth response gene 1 (Egr-1) levels in HMEC-Ls, and reduced the levels of Egr-1 on the FGF2 promoter.
Reference: Angiogenesis. 2012 Mar;15(1):99-114. https://pubmed.ncbi.nlm.nih.gov/22198237/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| Ethanol |
4.5 |
10.00 |
|
| PBS (pH 7.2) |
0.3 |
0.66 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
451.39
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Cao YJ, Surowy CS, Puttfarcken PS. Different nicotinic acetylcholine receptor subtypes mediating striatal and prefrontal cortical [3H]dopamine release. Neuropharmacology. 2005 Jan;48(1):72-9. doi: 10.1016/j.neuropharm.2004.09.005. PMID: 15617729.
2. Maggi L, Palma E, Eusebi F, Moretti M, Balestra B, Clementi F, Gotti C. Selective effects of a 4-oxystilbene derivative on wild and mutant neuronal chick alpha7 nicotinic receptor. Br J Pharmacol. 1999 Jan;126(1):285-95. doi: 10.1038/sj.bjp.0702299. PMID: 10051147; PMCID: PMC1565803.
3. Brown KC, Lau JK, Dom AM, Witte TR, Luo H, Crabtree CM, Shah YH, Shiflett BS, Marcelo AJ, Proper NA, Hardman WE, Egleton RD, Chen YC, Mangiarua EI, Dasgupta P. MG624, an α7-nAChR antagonist, inhibits angiogenesis via the Egr-1/FGF2 pathway. Angiogenesis. 2012 Mar;15(1):99-114. doi: 10.1007/s10456-011-9246-9. Epub 2011 Dec 25. Erratum in: Angiogenesis. 2012 Jun;15(2):331. Dosage error in article text. PMID: 22198237.
4. Gotti C, Balestra B, Moretti M, Rovati GE, Maggi L, Rossoni G, Berti F, Villa L, Pallavicini M, Clementi F. 4-Oxystilbene compounds are selective ligands for neuronal nicotinic alphaBungarotoxin receptors. Br J Pharmacol. 1998 Jul;124(6):1197-206. doi: 10.1038/sj.bjp.0701957. PMID: 9720791; PMCID: PMC1565512.
In vitro protocol:
1. Cao YJ, Surowy CS, Puttfarcken PS. Different nicotinic acetylcholine receptor subtypes mediating striatal and prefrontal cortical [3H]dopamine release. Neuropharmacology. 2005 Jan;48(1):72-9. doi: 10.1016/j.neuropharm.2004.09.005. PMID: 15617729.
2. Maggi L, Palma E, Eusebi F, Moretti M, Balestra B, Clementi F, Gotti C. Selective effects of a 4-oxystilbene derivative on wild and mutant neuronal chick alpha7 nicotinic receptor. Br J Pharmacol. 1999 Jan;126(1):285-95. doi: 10.1038/sj.bjp.0702299. PMID: 10051147; PMCID: PMC1565803.
In vivo protocol:
1. Brown KC, Lau JK, Dom AM, Witte TR, Luo H, Crabtree CM, Shah YH, Shiflett BS, Marcelo AJ, Proper NA, Hardman WE, Egleton RD, Chen YC, Mangiarua EI, Dasgupta P. MG624, an α7-nAChR antagonist, inhibits angiogenesis via the Egr-1/FGF2 pathway. Angiogenesis. 2012 Mar;15(1):99-114. doi: 10.1007/s10456-011-9246-9. Epub 2011 Dec 25. Erratum in: Angiogenesis. 2012 Jun;15(2):331. Dosage error in article text. PMID: 22198237.
2. Gotti C, Balestra B, Moretti M, Rovati GE, Maggi L, Rossoni G, Berti F, Villa L, Pallavicini M, Clementi F. 4-Oxystilbene compounds are selective ligands for neuronal nicotinic alphaBungarotoxin receptors. Br J Pharmacol. 1998 Jul;124(6):1197-206. doi: 10.1038/sj.bjp.0701957. PMID: 9720791; PMCID: PMC1565512.
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).
