L755507 - Adrenergic Receptor Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEL755507Cat. No.: HY-19334CAS No.: 159182-43-1分式: CHNOS分量: 584.73作靶點(diǎn): Adrenergic Receptor; CRISPR/Cas9作通路: GPCR/G Protein; Neuronal Signaling; Cell Cycle/DNADamage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (213.77 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7102 mL 8.5510 mL 17.1019 mL5 mM 0.3420 mL 1.7102 mL 3.4204 mL10 mM 0.1710 mL 0.8551 mL 1.7102 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 L755507個(gè)有效的,

3、 選擇性強(qiáng)的 3-AR 激動(dòng)劑, 其 IC50 值為 35 nM。IC50 & Target IC50: 35 nM (3-AR) 1體外研究L755507 causes a robust concentration-dependent increase in cAMP accumulation (pEC50 values of 8.5and 12.3, respectively). Maximal cAMP accumulation with zinterol and L755507 is increased after1/2 Master of Small Molecules 您邊的抑制劑

4、師www.MedChemEpretreatment with pertussis toxin. In contrast to cAMP, zinterol, L755507 and L748337 increasephosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2) with very high potency (pEC50 values of10.9, 11.7 and 11.6) 1. L755507 and Scr7 do not reduce cell viability significantly.

5、 Scr7 does not affect cellcycle distribution in a range of 10 to 200M. L755507 significantly decreases the proportion of cells in theG2/M phase at 10M or 40M and increases the S-phase cells at 10M compare with the DMSO-treatedcells 2.PROTOCOLCell Assay 1 The cytosensor microphysiometer is used to me

6、asure 3-AR-mediated increases in ECAR . In brief, CHO 3cells are seeded into 12-mm Transwell inserts at 5105 cells/cup and left to adhere overnight. On the day ofexperiment, cells are equilibrated for 2 h, and cumulative concentration-response curves to L755507,zinterol, or L748337 are constructed i

7、n paired sister cells with each concentration of drug exposed to cells for14 min. Results are expressed as a percentage of the maximal response to L755507. In experimentsexamining the effect of inhibitors, cells are treated for 30 min before stimulation with appropriate drugs. Alldrugs are diluted i

8、n modified RPMI 1640 medium. These results are expressed as a percentage of themaximal response to L755507, zinterol, or L748337 over basal 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sato M, et al. The beta3-adrenoceptor agonist 4-(H

9、exylamino)carbonylamino-N-4-2-(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propylaminoethyl-phenyl-benzenesulfonamide (L755507) and antagonist (S)-N-4-2-3-3-(acetamidomethyl)phenoxy-2-hydroxypropylamino-ethylphenylbenzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1cells stably expressing the human beta3-adrenoceptor. Mol Pharmacol. 2008 Nov;74(5):1417-28.2. Guoling Li, et al. Small molecules enhance CRISPR/Cas9-mediated homology-directed genome editing in primary cells. Sci Rep. 2017;7: 8943.McePdfHeightCaution: Product has not been fully validat