PMX 205 acetate(514814-49-4 free base) 是补体 C5a 受体 (C5aR; CD88) 的拮抗剂。
产品描述
PMX 205 acetate is an antagonist of complement C5a receptor (C5aR; CD88).
体外活性
PMX 205 (PMX205) group is in between 0.09893 to 0.2465, EP54 group, 0.02724 to 0.1748 and Tamoxifen group, the value recorded in between 0.09880 to 0.2464. For the 48 h plate of incubation time, only two groups of PMX 205 and Tamoxifen show a significant result. The values recorded are in between 0.04987 to 0.3273 and 0.5777 to 0.8551 respectively. For the 72 h plate, only one group shows a significant result, PMX 205 (antagonist group) with the value recorded in between 0.02136 to 0.5322[1].
体内活性
Tg2576 mice are treated with PMX 205 (PMX205) at 20 μg/mL in the drinking water (n=17) from 12 to 15 mo of age, the time frame at which there is a rapid accumulation of amyloid deposits in these animals. Untreated Tg2576 animals (n=11) are used as controls. After 3 mo, animals treated with PMX 205 show significantly less fibrillar plaque load (thioflavine reactivity) than do untreated animals. In 3×Tg mice, PMX 205 also significantly reduces hyperphosphorylated tau (69%)[2].
Cas No.
T12506L1
分子式
C47H66N10O8
分子量
899.09
储存和溶解度
DMSO:60 mg/ml (66.73 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years