DAMGO - Opioid Receptor Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDAMGOCat. No.: HY-P0210CAS No.: 78123-71-4分式: CHNO分量: 513.59Sequence: Tyr-d-Ala-Gly-Me-Phe-Gly-olSequence Shortening: Y-d-Ala-G-Me-Phe-G-ol作靶点: Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Protect from lightPowder

2、-80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 33.33 mg/mL (64.90 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9471 mL 9.7354 mL 19.4708 mL5 mM 0.3894 mL 1.9471 mL 3.8942 mL10 mM 0.1947 mL 0.9735 mL 1.9471 mL请根据产品在不同溶剂

3、中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (4.87 mM); C

4、lear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.87 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.87 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DAMGO种选择性的 -阿受体 (-OPR) 激动剂。IC50 & Target Kd: 3.460.84 nM (native -OPR) 1体外研究 DAMGO, a

5、-opioid receptor selective agonist, distinguishes between - and -opioid receptors around theirfirst extracellular loops. In native -OPR, the Kd value for DAMGO is 3.46 0.84 nM (n=3). The chimericreceptor MMDD, in which the carboxy-terminal half of -OPR is replaced with the corresponding region of -O

6、PR, exhibits an equivalent affinity (Kd=2.130.40 nM; n=3) to DAMGO compared with the native -OPR 1.DAMGO is a selective -opioid peptide. DAMGO abolishes the neuroprotective effect of CXCL12 in N-methyl-d-aspartate (NMDA) neurotoxicity studies. Regulation of neuronal response to CXCL12 is essentialfo

7、r shaping of developing and mature central nervous system (CNS). To establish whether DAMGO alter theeffect of CXCL12 on neuronal survival, the ability of CXCL12 to protect neurons from N-methyl-d-aspartate(NMDA)-induced death is examined in the presence and absence of DAMGO. Cortical cultures are t

8、reatedwith DAMGO (1 and 10 M). Neurons are subsequently exposed to NMDA (20 min) and/or CXCL12 (added10 min before NMDA) in the absence of glia and then returned to the original culture dishes with the glialfeeder layer. Neuronal death is evaluated after 24 h. DAMGO inhibits neuronal survival promot

9、ed by CXCL122.PROTOCOLCell Assay 2 Neurons (9 days in vitro) are treated with DAMGO (10 M) for 24 h in their original culture dish, subsequentlytransferred to a dish containing Mg2+-free saline with glycine (15 M), and exposed to NMDA (100 M)and/or CXCL12 (20 nM) in absence of glia. After treatments

10、, neurons are moved back into the original culturedishes containing glia. Neuronal death is evaluated after 24 h. Hoechst 33342 (3 g/mL) combined withcleaved caspase-3 (1:100) staining is used to identify normal and apoptotic cells 2.MCE has not independently confirmed the accuracy of these methods.

11、 They are for reference only.REFERENCES1. FEBS Lett. 1995 Jan 2;357(1):93-7. Onogi T, et al. DAMGO, a mu-opioid receptor selective agonist, distinguishes between mu- anddelta-opioid receptors around their first extracellular loops.2. Patel JP, et al. Modulation of neuronal CXCR4 by the micro-opioid agonist DAMGO. J Neurovirol. 2006 Dec;12(6):492-500.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has