Endomorphin 1 acetate

Research use only, not for human use.

Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects.

Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties.

Endomorphin 1 acetate 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) acetate increases interleukin-8 secretion in Caco-2 cells. Endomorphin 1 (1 μM) acetate inhibits excitatory transmission in adult rat substantia gelatinosa neurons.

Endomorphin 1 (i.c.v.) acetate shows antinociceptive properties in mice, with an ED50 value of 6.16 nM.Endomorphin 1 (50 μg/kg, i.v., rats) acetate 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.

——

Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

——

——

1276123-71-7

670.75

C36H42N6O7

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (186.36 mM; Ultrasonic )

C(C)(O)=O.C([C@H](NC(=O)[C@H]1N(C([C@H](CC2=CC=C(O)C=C2)N)=O)CCC1)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)C=4C=5C(NC4)=CC=CC5

——

(-20℃)

With Ice Pack

≥ 2 years