Desformylflustrabromine-hydrochloride-Deformylflustrabromine-hydrochloride-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): nAChR作通路: Membrane Transporter/Ion Channel; Neuronal Signali

2、ng儲(chǔ)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(shí)驗(yàn) 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制備儲(chǔ)備液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。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.99 mM)

4、; Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.99 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.99 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Desformylflustrabromine hydrochlor

5、ide個(gè)有選擇性的 42 神經(jīng)元煙堿酰膽堿受體 (nAChR) 激動(dòng)劑，其 pEC50 值為 6.48。IC50 & Target 42 nAChR體外研究 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