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EM574

Motilin receptor agonist
 
ALX-380-264-M001 1 mg 310.00 USD
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Agonist of the motilin receptor. Shows antimicrobial and gastrointestinal motor stimulating activity in vitro and in vivo. Stimulates contractions of muscle strips in a concentration-dependent manner (10-7-10-5M) and this contractile effect is unaffected by pretreatment with atropine or tetrodotoxin (Prod. No. Prod. No. BML-NA120). Binds to smooth muscle homogenates wit a Kd value of 7.8 x 10-9. Has orexigenic activity with affinity for the growth-hormone secretagogue receptor (GHS-R, Ghrelin Receptor).

Product Specification

Alternative Name:Motilide, Idremcinal, 8,9-Didehydro-N-demethyl-9-deoxo-6-deoxy-6,9-epoxy-N-(1-methylethyl)-erythromycin
 
Formula:C39H69NO12
 
MW:744.0
 
Source:Semisynthetic from erythromycin A.
 
CAS:110480-13-2
 
Purity:≥95% (HPLC)
 
Appearance:White to off-white powder.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
380-264
380-264 1
Figure 1: Gastrointestinal contraction induced by EM574 (30μg/kg).
380-264 2
Figure 2: Displacement of iodinated motilin binding by motilides.
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Product Literature References

EM574, an erythromycin derivative, improves delayed gastric emptying of semi-solid meals in conscious dogs: F. Sato, et al.; Eur. J. Pharmacol. 395, 165 (2000), Abstract;
Effects of EM574 and cisapride on gastric contractile and emptying activity in normal and drug-induced gastroparesis in dogs: T. Tanaka, et al.; J. Pharmacol. Exp. Ther. 287, 712 (1998), Abstract;
EM574, an erythromycin derivative, is a motilin receptor agonist in the rabbit: F. Sato, et al.; Eur. J. Pharmacol. 322, 63 (1997), Abstract;
Bioactive metabolites of EM574 and EM523, erythromycin derivatives having strong gastrointestinal motor stimulating activity: Y. Funabashi, et al.; J. Antibiot. 49, 794 (1996), Abstract;
Vagus-dependent and vagus-independent mechanisms of action of the erythromycin derivative EM574 and motilin in dogs: N. Inatomi, et al.; Jpn. J. Pharmacol. 71, 29 (1996), Abstract;
EM574, an erythromycin derivative, is a potent motilin receptor agonist in human gastric antrum: M. Satoh, et al.; J. Pharmacol. Exp. Ther. 271, 574 (1994), Abstract;
Motilides, macrolides with gastrointestinal motor stimulating activity. I. O-substituted and tertiary N-substituted derivatives of 8,9-anhydroerythromycin A 6,9-hemiacetal: K. Tsuzuki, et al.; Chem. Pharm. Bull. 37, 2687 (1989), Abstract;
Macrolides with gastrointestinal motor stimulating activity: S. Omura, et al.; J. Med. Chem. 30, 1941 (1987), Abstract;
Gastrointestinal motor-stimulating activity of macrolide antibiotics and the structure-activity relationship: S. Omura, et al.; J. Antibiot. 38, 1631 (1985), Abstract;

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