Endomorphin 2;(Synonyms: 内吗啡肽 2)
Endomorphin 2,一种高度选择性的高亲和力μ-opioid受体激动剂 , 对kappa3结合位点具有高亲和力 ,Ki为 20 到 30 nM 之间。
Endomorphin 2 Chemical Structure
CAS No. : 141801-26-5
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Endomorphin 2 的其他形式现货产品:
生物活性 |
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] |
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体外研究 (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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
571.67 |
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Formula |
C32H37N5O5 |
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CAS 号 |
141801-26-5 |
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Sequence |
Tyr-Pro-Phe-Phe-NH2 |
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Sequence Shortening |
YPFF-NH2 |
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中文名称 |
内吗啡肽 2 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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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:
3.;;Recommended solution:
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参考文献 |
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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. |
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Animal Administration [1] |
Mice[1] MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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