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

Endomorphin 2 (Synonyms: Tyr-Pro-Phe-Phe-NH2; YPFF-NH2)

Cat. No.: HY-P0186
Handling Instructions

Endomorphin 2, 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 2 Chemical Structure

Endomorphin 2 Chemical Structure

CAS No. : 141801-26-5

Size Inquiry
5 mg Get quote for price and lead time
10 mg Get quote for price and lead time
25 mg Get quote for price and lead time

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

Endomorphin 2, 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 2 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 1 (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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.7493 mL 8.7463 mL 17.4926 mL
5 mM 0.3499 mL 1.7493 mL 3.4985 mL
10 mM 0.1749 mL 0.8746 mL 1.7493 mL
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
Molecular Weight

571.67

Formula

C₃₂H₃₇N₅O₅

CAS No.

141801-26-5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Endomorphin 2
Cat. No.:
HY-P0186
Quantity: