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 Details
| Alternative Name: | Motilide, Idremcinal, 8,9-Didehydro-N-demethyl-9-deoxo-6-deoxy-6,9-epoxy-N-(1-methylethyl)-erythromycin |
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| Formula: | C39H69NO12 |
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| MW: | 744.0 |
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| Source: | Semisynthetic from erythromycin A. |
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| CAS: | 110480-13-2 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | White to off-white powder. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Figure 1: Gastrointestinal contraction induced by EM574 (30μg/kg).
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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