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Cat. No.: HY-P0186

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Endomorphin 2

Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

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

CAS No.: 141801-26-5
Formula: C₃₂H₃₇N₅O₅
Molecular Weight:571.67

Storage:

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

Endomorphin 2 Chemical Structure

CAS No.: 141801-26-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

IC₅₀ & Target

μ Opioid Receptor/MOR

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.04 nM Compound: 6, Endomorphin-2	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	[PMID: 17266203]
CHO	EC₅₀	>1000 nM Compound: 6, Endomorphin-2	Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	[PMID: 17266203]
CHO	EC₅₀	0.04 nM Compound: 1, endomorphin-2	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	[PMID: 18207400]
CHO	EC₅₀	>1000 nM Compound: 1, endomorphin-2	Antagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay Antagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	[PMID: 18207400]
HEK293	EC₅₀	11.8 nM Compound: 2, EM-2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	[PMID: 22724433]
HEK293	EC₅₀	55.5 nM Compound: EM-2	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	[PMID: 32199689]

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 K_i 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 K_i values greater than 500 nM^[1].

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

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. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice^[1].

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

Chemical Information

CAS No. 141801-26-5
Molecular Weight 571.67
Formula C₃₂H₃₇N₅O₅
Sequence

Tyr-Pro-Phe-Phe-NH2
Sequence Shortening

YPFF-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Solvent & Solubility

In Vitro

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References

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Endomorphin 2

All Opioid Receptor Isoforms

Biological Activity

Description

IC50 & Target

Cellular Effect

In Vitro

In Vivo

Chemical Information

Solvent & Solubility

In Vitro

Purity & Documentation

References

Calculators

Help & FAQs

Endomorphin 2 Related Classifications

HY-P0186 Related Classifications

Bioz

Keywords

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