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674786-20-0

中文名稱 化合物 T11044
英文名稱 Dihydromunduletone
CAS 674786-20-0
分子式 C25H28O6
分子量 424.49
MOL 文件 674786-20-0.mol
674786-20-0 結(jié)構(gòu)式 674786-20-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11044
英文別名
Dihydromunduletone

物理化學(xué)性質(zhì)

沸點(diǎn)615.9±55.0 °C(Predicted)
密度1.223±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 250 mg/mL (588.94 mM)
酸度系數(shù)(pKa)7.70±0.60(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
化合物 T11044價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/05/22HY-101483化合物 T11044
Dihydromunduletone
674786-20-01 mg2200元
2025/05/22HY-101483化合物 T11044
Dihydromunduletone
674786-20-05mg5500元
2025/05/22HY-101483化合物 T11044
Dihydromunduletone
674786-20-010mM * 1mLin DMSO6050元

常見(jiàn)問(wèn)題列表

生物活性
Dihydromunduletone (DHM) 是類胡蘿卜素衍生物,是一種選擇性,有效的粘附 G 蛋白偶聯(lián)受體 (aGPCR) (GPR56 and GPR114/ADGRG5) 拮抗劑,對(duì) GPR56 的 IC 50 值為 20.9 μM,但不抑制 GPR110 或 A 類 GPCR。
靶點(diǎn)

IC50: 20.9 μM (GPR56); GPR114

體外研究

Assays are initiated by the addition of [ 35 S]GTPγS, and the rates of aGPCR-stimulated G protein activation ([ 35 S]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 (50 μM), the rate of GPR114 7TM-stimulated Gs activity is also inhibited dramatically. When Dihydromunduletone (50 μM) 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 3 μM 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 synthetic-peptide agonist and tethered-peptide agonist-mediated aGPCR activation in isolated membranes and HEK293T cell-based assays, but it does not inhibit basal receptor signaling.

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