Desformylflustrabromine-hydrochloride-Deformylflustrabromine-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDesformylflustrabromine hydrochlorideCat. No.: HY-107675CAS No.: 951322-11-5Synonyms: Deformylflustrabromine hydrochloride; dFBr hydrochloride分式: CHBrClN分量: 357.72作靶点: nAChR作通路: Membrane Transporter/Ion Channel; Neuronal Signali

2、ng储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 105 mg/mL (293.53 mM)H2O : 5 mg/mL (13.98 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7955 mL 13.9774 mL 27.9548 mL5 mM 0.5591 mL 2.7955 mL 5.

3、5910 mL10 mM 0.2795 mL 1.3977 mL 2.7955 mL请根据产品在不同溶剂中的溶解度，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% salineSolubility: 2.5 mg/mL (6.99 mM)

4、; Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.99 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.99 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Desformylflustrabromine hydrochlor

5、ide个有选择性的 42 神经元烟碱酰胆碱受体 (nAChR) 激动剂，其 pEC50 值为 6.48。IC50 & Target 42 nAChR体外研究 Desformylflustrabromine hydrochloride is a selective agonist of 42 neuronal nicotinic acetylcholinereceptor (nAChR) with a pEC50 of 6.48 1. ACh-induced currents are potentiated and inhibited byDesformylflustrabromine hydr

6、ochloride in the high sensitivity (HS) and low sensitivity (LS) isoformpreparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform(pEC50=6.40.2) compare with the HS isoform (pEC50=5.60.2). Desformylflustrabromine hydrochloridepotentiates ACh-induced respo

7、nses of wild-type receptors expressed using the HS isoform preparationmaximally by 35020%, which is similar to receptors expressed via the LS isoform preparation (35030%)2.PROTOCOLKinase Assay 2 Receptors expressed via the high sensitivity (HS) isoform preparation are evaluated forDesformylflustrabr

8、omine hydrochloride modulation by coapplication of 10 M ACh with increasingconcentrations of Desformylflustrabromine hydrochloride (0.001 to 100 M). To compare responses fromdifferent oocytes, individual responses to Desformylflustrabromine hydrochloride application are normalizedto the control resp

9、onses elicited using either 10 or 100 M ACh for receptors expressed by the HS or LSisoform preparations, respectively, for both wild-type and mutated receptors. Data are collected from at leastfour replicate experiments using oocytes obtained from at least two different frogs 2.MCE has not independe

10、ntly confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Nadezhda German, et al. Deconstruction of the 42 Nicotinic Acetylchloine (nACh) Receptor Positive Allosteric Modulator des-Formylflustrabromine (dFBr). J Med Chem. 2011 Oct 27;54(20):7259-67.2. Weltzin MM, et al. Desformylflustrabromine Modulates 42 Neuronal Nicotinic Acetylcholine Receptor High- and Low-SensitivityIsoforms at Allosteric Clefts Containing the 2 Subunit. J Pharmacol Exp Ther. 2015 Aug;354(2):184-94.McePdfHeightCaution: Product has not been