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製品番号: 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.

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CAS 番号: 141801-26-5
分子式: C₃₂H₃₇N₅O₅
分子量:571.67

保管条件:

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

Endomorphin 2 構造式

CAS 番号: 141801-26-5

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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

Opioid Receptor アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 141801-26-5
分子量 571.67
分子式 C₃₂H₃₇N₅O₅
配列

Tyr-Pro-Phe-Phe-NH2
シーケンスの短縮

YPFF-NH2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

溶剤 & 溶解度

体外

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.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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