化合物 T11044
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- CAS号:
- 674786-20-0
- 英文名:
- Dihydromunduletone
- 英文别名:
- Dihydromunduletone;Ethanone, 1-(3,4-dihydro-3,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-2-(5-methoxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-
- 中文名:
- 化合物 T11044
- 中文别名:
- 化合物 T11044
- CBNumber:
- CB24667823
- 分子式:
- C25H28O6
- 分子量:
- 424.49
- MOL File:
- 674786-20-0.mol
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化合物 T11044化学性质
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沸点:
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615.9±55.0 °C(Predicted)
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密度:
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1.223±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 250 mg/mL (588.94 mM)
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酸度系数(pKa):
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7.70±0.60(Predicted)
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化合物 T11044性质、用途与生产工艺
Dihydromunduletone (DHM) 是类胡萝卜素衍生物,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 20.9 μM,但不抑制 GPR110 或 A 类 GPCR。
IC50: 20.9 μM (GPR56); GPR114
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.
化合物 T11044
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-101483 | Dihydromunduletone | | 1 mg | 2200元 |
2024/01/25 | HY-101483 | 化合物 T11044 Dihydromunduletone | 674786-20-0 | 5mg | 5500元 |
674786-20-0, 化合物 T11044 相关搜索:
- 化合物 T11044
- 674786-20-0
- Ethanone, 1-(3,4-dihydro-3,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-2-(5-methoxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-
- Dihydromunduletone