914291-61-5
914291-61-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12567 英文別名
PS3724243-Isoquinolinecarboxamide, N-[(1S)-4-[(aminoiminomethyl)amino]-1-[[(cyclohexylmethyl)amino]carbonyl]butyl]-2-(1,4-dioxo-4-phenylbutyl)-1,2,3,4-tetrahydro-, (3S)-
物理化學(xué)性質(zhì)
密度1.29±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.47±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
PS372424，CXCL10 的三個(gè)氨基酸片段，是一種特異的人 CXCR3 激動(dòng)劑，具有抗炎活性。在關(guān)節(jié)炎炎癥模型中，PS372424 可抑制 T 細(xì)胞遷移。靶點(diǎn)
|
Human CXCR3
|
體外研究
PS372424 (100?ng/mL) increases p-Erk1 and p-Erk2 in U87-CXCR3-A cells after 5?min of stimulation.
PS372424 (10-200 nM; 30 min) causes a concentration-dependent phosphorylation of CCR5 on CXCR3
+
T cells not in CXCR3
-
T cells.
PS372424 competes for binding of radiolabeled CXCL10 to membranes prepared from HEK293/CXCR3 Gqi5 cells with an IC
50
of 42±21 nM.
Western Blot Analysis
| Cell Line: | CXCR3 + T cells and CXCR3 - T cells |
| Concentration: | 10, 50, 100, or 200 nM |
| Incubation Time: | 30 minutes |
| Result: | Caused a concentration-dependent phosphorylation of CCR5 on CXCR3 + T cells. Did not result in phosphorylation of CCR5 on CXCR3 - T cells. |