Dihydromunduletone  ≥98%

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包装规格:5mg 10mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(250mg/mL超声)
产品描述:基本信息 产品编号: D11349 产品名称: Dihydromunduletone CAS: 674786-20-0   储存条件 粉末 -20℃ 四年     分子式: C25H28O6 溶于液体 -80℃ 六个月 分子量 424.49 -20℃ 一个月 化学名:  1-(3,7-dihydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)-2-(5-methoxy-2,2-dimethyl-1-benzopyran-6-yl)ethanone Solubility (25°C):   体外:   DMSO 250mg/mL (588.94mM; Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.08mg/mL (4.90mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (4.90mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08mg/mL (4.90mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (4.90mM,饱和度未知) 的澄清溶液。以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.08mg/mL (4.90mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (4.90mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3558mL 11.7788mL 23.5577mL 5mM 0.4712mL 2.3558mL 4.7115mL 10mM 0.2356mL 1.1779mL 2.3558mL   生物活性 产品描述 类胡萝卜素衍生物,是一种选择性,有效的粘附 G 蛋白偶联受体 (aGPCR) (GPR56 and GPR114/ADGRG5) 拮抗剂,对 GPR56 的 IC 50 值为 20.9μM,但不抑制 GPR110 或 A 类 GPCR。 靶点 IC50: 20.9μM (GPR56); GPR114 体外研究 Assays are initiated by the addition of [35S]GTPγS, and the rates of aGPCR-stimulated G protein activation ([35S]GTPγS binding to Gα) are measured with or without the influence of added compounds. Dihydromunduletone (DHM) inhibits the kinetics of GPR56 7TM-stimulated G13 GTPγS binding to varying degrees. Dihydromunduletone is the best inhibitory compound and reduced the rate at which GPR56 7TM activated G13 >75% (from 0.18 to 0.04 minute−1). At a concentration of Dihydromunduletone (DHM) that maximally inhibits GPR56 (50μM), the rate of GPR114 7TM-stimulated Gs activity is also inhibited dramatically. When Dihydromunduletone (50μM) is applied to the GPR110 7TM, it fails to inhibit GPR110 stimulation of Gq GTPγS binding. Cells transfected with GPR56 A386M 7TM are incubated with increasing concentrations of Dihydromunduletone. P7 peptide agonist is added, and SRE-luciferase activity is measured. Dihydromunduletone inhibits the P7 peptide-induced luciferase activity in a concentration-dependent manner. Cells are also treated with a fixed concentration of 3μM Dihydromunduletone and then stimulated with an increasing concentration of P7 peptide agonist. Dihydromunduletone treatment blunts P7 peptide activation at each concentration. In conclusion, Dihydromunduletone antagonizes syntheticpeptide agonist and tethered-peptide agonist-mediated aGPCR activation in isolated membranes and HEK293T cell-based assays, but it does not inhibit basal receptor signaling
保存条件:-20℃