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Dimethyl-W84 dibromide

M2 receptor modulator
ALX-550-400-M005 5 mg 170.00 USD
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Very potent allosteric modulator of muscarinic receptors, selective for M2-receptors. Retards the dissociation of the antagonist N-methylscopolamine. Affinity for the free receptor is about 10-fold higher than with W84 (Prod. No. ALX-550-399). pKA=7.08, p(αKA)=6.75, pEC50,diss=6.77.

Product Details

Alternative Name:N,N’-Bis[3-(1,3-dihydro-5-methyl-1,3-dioxo-2H-isoindol-2-yl)propyl]-N,N,N’,N’-tetramethyl-1,6-hexanediamminium dibromide
Purity:≥98% (HPLC)
Appearance:White to off-white solid.
Solubility:Soluble in DMSO, water or aqueous buffer.
Shipping:Ambient Temperature
Long Term Storage:+4°C
Handling:Avoid freeze/thaw cycles.
Regulatory Status:RUO - Research Use Only
ALX-550-400 structure
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ALX-550-400 structure

Product Literature References

Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors: C. Trankle, et al.; Mol. Pharmacol. 68, 1597 (2005), Abstract;
Allosteric site on muscarinic acetylcholine receptors: identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupie: U. Voigtlander, et al.; Mol. Pharmacol. 64, 21 (2003), Abstract; Full Text
Contribution of lateral substituents in symmetrical and non-symmetrical heptane-bisammonio compounds to the allosteric stabilization of N-methylscopolamine binding to muscarinic M2 receptors: M. Staudt, et al.; Arch. Pharm. (Weinheim) 336, 385 (2003), Abstract;
Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 64, 180 (2003), Abstract; Full Text
Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators: A. Raasch, et al.; J. Med. Chem. 45, 3809 (2002), Abstract;
Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties: R. Li, et al.; Arch. Pharm. 334, 121 (2001), Abstract;
Using a radioalloster to test predictions of the cooperativity model for gallamine binding to the allosteric site of muscarinic acetylcholine M(2) receptors: C. Trankle, et al.; Mol. Pharmacol. 56, 962 (1999), Abstract; Full Text
Identification of a [3H]Ligand for the common allosteric site of muscarinic acetylcholine M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 54, 139 (1998), Abstract; Full Text

General Literature References

G protein-coupled receptor allosterism and complexing: A. Christopoulos and T. Kenakin; Pharmacol. Rev. 54, 323 (2002), Abstract;

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