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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESerotonin hydrochlorideCat. No.: HY-B1473CAS No.: 153-98-0Synonyms: 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride分式: CHClNO分量: 212.68作靶點: 5-HT Receptor; COMT作通路: GPCR/G Protein; Neuronal Signaling; MetabolicEnzyme/Protea
2、se儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 130 mg/mL (611.25 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.7019 mL 23.5095 mL 47.0190 mL5 mM 0.9404 mL 4.7019 mL 9.4038 mL10 mM 0.4702 mL 2.3510 mL 4.7019 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶
3、劑配制儲備液,并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?,再依次添加助溶?為保證實驗結(jié)果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當天使;澄清的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (12.13 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in sali
4、ne)Solubility: 2.58 mg/mL (12.13 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (12.13 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Serotonin hydrochloride是CNS 中的單胺神經(jīng)遞質(zhì)和內(nèi)源性 5-HT 受體激動劑。Serotonin hydrochloride 也茶
5、酚 O-甲基轉(zhuǎn)移酶 (COMT) 的抑制劑其 Ki 值為 44 M。IC50 & Target 5-HT receptor 1Ki: 44 M (COMT) 1體外研究 Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptoragonist. Serotonin hydrochloride also inhibits catechol O-methyltransferase (COMT), an enzyme thatcontributes to modu
6、ltion the perception of pain, via non-competitive binding to the site bound by catecholsubstrates with a binding affinity comparable to the binding affinity of catechol itself (Ki=44 M). Resultsshow that addition of 100 M of Serotonin hydrochloride decreases the reaction velocity of COMT 1.體內(nèi)研究 Sero
7、tonin hydrochloride produces robust hypersensitivity compare to saline-treated controls (p 1. Asignificant increase in colonic 5-HT content is observed in IL-13-/- mice receiving Serotonin hydrochloridecompare to IL-13-/- receiving vehicle following induction of DSS colitis 2.PROTOCOLCell Assay 2 Fo
8、r macrophage culture, peritoneal cavity cells are collected from WT and IL-13-/- mice with or withoutdextran sodium sulfate (DSS) treatment and cultured. Cells are plated at a concentration of 3.0106 cells permillilitre, and treated with either lipopolysaccharides (LPS); (100 ng/mL) or Serotonin hyd
9、rochloride (10-10 M)for 24 hours. The culture supernatant are collected and stored in -80C until determination of cytokine levelsusing protein array system 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Dextran sodium sulfate (DSS) colitis is
10、induced by orally administering 5% DSS in drinking water for 5 days.Administration 2 In a separate experiment, IL-13-/- mice are injected subcutaneously with 100 mg/kg of Serotoninhydrochloride (5-HTP) twice daily for 8 days beginning 3 days prior to induction of DSS colitis; whereas, thecontrol IL-
11、13-/- mice receive saline as vehicle. Animals are anaesthetized prior to euthanization via cervicaldislocation at the conclusion of each experiment or if they reach a predetermined end point (ie, loss of 20%body weight and/or significant deterioration of body condition) 2.MCE has not independently c
12、onfirmed the accuracy of these methods. They are for reference only.REFERENCES1. Tsao D, et al. Serotonin-induced hypersensitivity via inhibition of catechol O-methyltransferase activity. Mol Pain. 2012 Apr 13;8:25.2. Shajib MS, et al. Interleukin 13 and serotonin: linking the immune and endocrine systems in murine models of intestinal inflammation.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEPLoS One. 2013 Aug 28;8(8):e72774.McePdfHeightCau
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