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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 | PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM when tested with the FS-3 substrate. The efficacy of PF-8380 is sustained when the enzyme, derived from fetal fibroblasts, is combined with lysophosphatidyl choline (LPC) as the substrate. In human whole blood incubated with PF-8380 for 2 hours, autotaxin inhibition occurs with an IC50 of 101 nM[1]. Autotaxin (ATX), an enzyme with lysophospholipase D (lysoPLD) activity, converts lysophosphatidylcholine (LPC) into lysophosphatidic acid (LPA). Treatment of GL261 and U87-MG cells with 1 μM PF-8380 prior to 4 Gy irradiation leads to reduced clonogenic survival, lowered migration (33% in GL261; P=0.002 and 17.9% in U87-MG; P=0.012), decreased invasion (35.6% in GL261; P=0.0037 and 31.8% in U87-MG; P=0.002), and reduced radiation-induced Akt phosphorylation[2]. |
体内研究 | The pharmacokinetic properties of PF-8380 are assessed following an intravenous dose of 1 mg/kg and oral doses ranging from 1 to 100 mg/kg over a 24-hour period. PF-8380 exhibits a mean clearance rate of 31 mL/min/kg, a steady-state distribution volume of 3.2 L/kg, and an effective half-life of 1.2 hours. Its oral bioavailability is moderate, varying between 43 and 83%. Plasma concentrations rise with increasing single oral doses; however, the maximum concentration (Cmax) increases roughly proportionally with doses from 1 to 10 mg/kg and less than proportionally from 10 to 100 mg/kg. Drug exposure, as estimated by the area under the curve (AUC), is approximately proportional to the dose and remains linear up to 100 mg/kg. Levels of plasma C16:0, C18:0, and C20:0 LPA are measured immediately after collection. The most significant reduction in LPA levels occurs at the 3 mg/kg dose within 0.5 hours, with all LPA levels returning to or surpassing baseline by 24 hours[1]. Treatment with 10 mg/kg PF-8380 modestly increases tumor-associated vascularity by 20% (P=0.497). However, administering PF-8380 45 minutes before a 4 Gy irradiation reduces vascularity by nearly 48% compared to control (P=0.031), and by 65% relative to mice that underwent radiation alone (P=0.011)[2]. |
体外研究 | PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM when tested with the FS-3 substrate. The efficacy of PF-8380 is sustained when the enzyme, derived from fetal fibroblasts, is combined with lysophosphatidyl choline (LPC) as the substrate. In human whole blood incubated with PF-8380 for 2 hours, autotaxin inhibition occurs with an IC50 of 101 nM[1]. Autotaxin (ATX), an enzyme with lysophospholipase D (lysoPLD) activity, converts lysophosphatidylcholine (LPC) into lysophosphatidic acid (LPA). Treatment of GL261 and U87-MG cells with 1 μM PF-8380 prior to 4 Gy irradiation leads to reduced clonogenic survival, lowered migration (33% in GL261; P=0.002 and 17.9% in U87-MG; P=0.012), decreased invasion (35.6% in GL261; P=0.0037 and 31.8% in U87-MG; P=0.002), and reduced radiation-induced Akt phosphorylation[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.45mL 2.09mL 1.05mL |
20.91mL 4.18mL 2.09mL |
CAS号 | 1144035-53-9 |
分子式 | C22H21Cl2N3O5 |
分子量 | 478.325 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(219.52 mM),配合低频超声助溶,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 |
1%CMC Na +water 15 mg/mL suspension |