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ANQ 11125 Motilin receptor antagonist,selective

Catalog No.B5803
Size Price Stock Qty
1mg
$279.00
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

ANQ 11125

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Chemical Properties

Cas No. 153966-48-4 SDF Download SDF
Synonyms N/A
Chemical Name (2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S)-17-((Z)-((3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S,18Z,20S,21Z,23S)-23-amino-11,17-dibenzyl-14-((S)-sec-butyl)-1,4,7,10,13,16,19,22-octahydroxy-5-(4-hydroxybenzyl)-8-((R)-1-hydroxyethyl)-20-isopropyl-24-phenyl-3,6,9,12,15
Canonical SMILES CC[[email protected]]([[email protected]@](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](N)([H])CC1=CC=CC=C1)([H])C(C)C)([H])CC2=CC=CC=C2)([H])/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/C/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](C(O)=O)([H])CC
Formula C86H125N19O21 M.Wt 1761.05
Solubility Storage Store at -20°C
Physical Appearance White lyophilised solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

ANQ 11125 is a selective antagonist of motilin receptor with pKd of 8.24 [1].

Motilin receptor is a G protein-coupled receptor for motilin and stimulates contraction of gut smooth muscle.

ANQ 11125 is a selective motilin receptor antagonist. The affinity of ANQ 11125 for motilin receptor is about 10 times less than motilin [1]. In rabbit antral smooth muscle tissue, ANQ-11125 bound to motilin receptor with pKd value of 8.16. While, ANQ-11125 didn’t induce contractions of rabbit duodenum. ANQ-11125 (10-5 M) induced contractile response by 29% compared to ACh [2].

References:
[1].  Depoortere I, Macielag MJ, Galdes A, et al. Antagonistic properties of [Phe3,Leu13]porcine motilin. Eur J Pharmacol, 1995, 286(3): 241-247.
[2].  Peeters TL, Depoortere I, Macielag MJ, et al. The motilin antagonist ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit. Biochem Biophys Res Commun, 1994, 198(2): 411-416.