1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Endomorphin 1

Endomorphin 1 

Cat. No.: HY-P0185 Purity: 98.15%
Handling Instructions

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.

For research use only. We do not sell to patients.

Endomorphin 1 Chemical Structure

Endomorphin 1 Chemical Structure

CAS No. : 189388-22-5

Size Price Stock Quantity
10 mM * 1 mL in Water USD 67 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
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25 mg USD 120 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.

IC50 & Target

Ki: 20-30 nM (kappa3 opioid receptor)[1]

In Vitro

Endomorphin 1 (EM-1) is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 2 (EM-2). The two Endomorphins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ1 and μ2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM[1].

In Vivo

Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice[1].

Molecular Weight

610.70

Formula

C₃₄H₃₈N₆O₅

CAS No.

189388-22-5

Sequence

Tyr-Pro-Trp-Phe-NH2

Sequence Shortening

YPWF-NH2

SMILES

O=C(N)[[email protected]](CC1=CC=CC=C1)NC([[email protected]](CC2=CNC3=CC=CC=C23)NC([[email protected]]4N(C([[email protected]](CC5=CC=C(C=C5)O)N)=O)CCC4)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Protect from light, stored under nitrogen
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (40.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6375 mL 8.1873 mL 16.3747 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 mL
10 mM 0.1637 mL 0.8187 mL 1.6375 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2 nM) is performed in potassium phosphate buffer (50 mM, pH 7.4; 0.5 mL) with MgCl2 (5 mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06 mg protein/mL for MOR-1/CHO cells. Specific binding is determined in the presence and absence of either 1 μM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25°C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethylenimine and washed twice with ice cold Tris buffer using a Brandel cell harvester. The filters are then counted on a Packard Cobra gamma counter. The other opioid receptor binding assays are performed[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Groups of mice are treated i.c.v. with Endomorphin 1 (12 μg) or Endomorphin 2 (3 μg) 15 min before a 0.5-cc charcoal meal (2.5% gum tragacanth,10% activated charcoal in water). The mice are killed 30 min later and the distance the charcoal traveled is measured.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Endomorphin 1Endomorphin1Endomorphin-1Opioid ReceptorInhibitorinhibitorinhibit

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