Endomorphin-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Endomorphin 1 是 μ-阿片受体的高亲和力和选择性激动剂，对 kappa3 结合位点表现出合理的亲和力 (Ki: 20~30 nM)。

Endomorphin 1 is a high affinity and selective agonist of the μ-opioid receptor and displays reasonable affinities for kappa3 binding sites (Ki: 20~30 nM).

Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells.Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells.Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons.

Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM.Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response. Animal Model:ICR mice.Dosage:6.16 nM (ED50 Administration:Intracerebroventricularly (i.c.v.) injection Result:Inhibited dose-dependently the tail-flick response.Animal Model:Rats.Dosage:50 μg/kg Administration:Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.Result:Alleviated MIRI by reducing the production of free radicals.Dncreased LDH and CK-MB activities.Increased SOD activity and decreased MDA content.Decreased IL-6 and TNF-α plasma content.

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Endocrinology/Hormones

Opioid Receptor

μ-opioid receptor

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189388-22-5

610.67

C34H38N6O5

>98% (HPLC)

Water:24 mg/mL (39.3 mM; Need ultrasonic)

C1C[C@H](N(C1)C(=O)[C@H](CC2=CC=C(C=C2)O)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N

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(-20℃)

With Ice Pack

≥ 2 years