货号:A144892
同义名:
Luteoline;Luteolol
Luteolin 是一种天然黄酮,具有抗氧化、抗炎和抗癌活性。Luteolin 在研究中主要用于探索其在肿瘤抑制、心血管健康和神经保护方面的作用。
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产品名称 | PDE ↓ ↑ | PDE1 ↓ ↑ | PDE10A ↓ ↑ | PDE2 ↓ ↑ | PDE3 ↓ ↑ | PDE4 ↓ ↑ | PDE5 ↓ ↑ | PDE6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Doxofylline | ✔ | 99+% | |||||||||||||||||
Deltarasin |
+++
PDEδ , Kd: 38 nM |
99+% | |||||||||||||||||
7-(2,3-Dihydroxypropyl)theophylline | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
PF-2545920 |
++++
PDE10A, IC50: 0.37 nM |
97% | |||||||||||||||||
Luteolin |
+
PDE1, Ki: 15.0 μM |
++
PDE2, Ki: 6.4 μM |
+
PDE3, Ki: 13.9 μM |
+
PDE4, Ki: 11.1 μM |
+
PDE5, Ki: 9.5 μM |
98% | |||||||||||||
Milrinone |
++
PDE2, IC50: 5.2 μM |
++
PDE3, IC50: 2.1 μM |
ATPase | 99%+ | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Phosphodiesterases (PDEs) comprise 11 enzyme families that hydrolyze adenosine 3′,5′ cyclic monophosphate and/or guanosine 3′,5′ cyclic monophosphate. Luteolin is a flavonoid that has been shown to inhibit PDE1-5 with IC50 values of around 20μM. The Ki values of luteolin against PDE1-5 were 15.0 3.9, 6.4 1.9, 13.9 4.2, 11.1 3.7 and 9.5 1.7μM, respectively. The EC50 (PDE4H) value of luteolin for displacing 2nM [3H]-rolipram binding on the high-affinity rolipram binding sites was 11.2 ± 1.5μM[9]. In RAW 264.7 cells, luteolin inhibited LPS-induced TNF-alpha release with an IC50 value of less than 1μM. Preincubation of cells with luteolin also inhibited LPS-induced phosphorylation of Akt and IkappaB-alpha[10]. Treatment with luteolin (10 – 30μmol/kg, s.c.) significantly and dose-dependently shortened the duration of xylazine/ketamine-induced anesthesia. Also, luteolin inhibited 5nM [3H]-flunitrazepam binding to rat cerebral cortex membranes with a Ki value of 60.1μM[9]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
CHO cells | Function assay | Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 μM | 20971650 | ||
HEK293 cells | Function assay | 24 h | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=2.3 μM | 24955889 | |
HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=0.85 μM | 20731357 | ||
HL60 cells | 30 μM | Proliferation assay | 48 h | Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay | 18258440 |
Dose | Mice: 0.2 mg/kg - 1 mg/kg[3] (i.p.), 5 mg/kg - 20 mg/kg[4] (i.p.); 0.1 mg/kg - 0.3 mg/kg[5] (i.g.); 0.1 mg/kg - 10 mg/kg[6] (p.o.) Rat: 50 mg/kg[7] (i.v.); 5 mg/kg - 20 mg/kg[8] (i.p.) | ||||||||||||||||
Administration | i.p., i.g., p.o., i.v. | ||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.49mL 0.70mL 0.35mL |
17.47mL 3.49mL 1.75mL |
34.94mL 6.99mL 3.49mL |
CAS号 | 491-70-3 |
分子式 | C15H10O6 |
分子量 | 286.24 |
别名 | Luteoline;Luteolol;Salifazide;Flacitran;Cyanidenon 1470;CCRIS 3790;C.I. Natural Yellow 2;C.I. 75590;BRN 0292084;Digitoflavone |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(366.83 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |