丙酸倍氯松二溴酸盐
丙酸倍氯松二溴酸盐 性质
| 熔点 | 205°C(lit.) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：30mg/mL；乙醇：2.5mg/mL；水：20mg/mL |
| 形态 | 粉末晶体 |
| 颜色 | 白色到灰色到红色 |
| 水溶解性 | Soluble to 100 mM in water |
丙酸倍氯松二溴酸盐 用途与合成方法
|
Human H3LR 9.44 (pKi) |
Rat H3LR 9.75 (pKi) |
H 4 receptor 13 nM (Ki) |
H 2 Receptor 5.6 (pKi) |
Clobenpropit binds to human H3LR and rat H3LR with pK
i
s of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pK
i
s of 5.2 and 5.6, respectively).
Clobenpropit inhibits [
3
H]-dopamine transport by SH-SY5Y cells in a concentration dependent manner with maximum inhibition 82.7±2.8 % and IC
50
490 nM (pIC
50
6.31±0.11).
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC
50
1 μM for the NR1/NR2B receptor).
Clobenpropit (50 μM) and Gemcitabine (5 μM) combination therapy significantly increases apoptosis of Panc-1, MiaPCa-2 and AsPC-1 compared with control.
Apoptosis Analysis
| Cell Line: | Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1) |
| Concentration: | 50 μM |
| Incubation Time: | |
| Result: | Enhanced apoptotic cell death in combination of Gemcitabine (5 μM). |
The combination treatment of Clobenpropit (every other day intraperitoneal injection at 20 μM per kilogram for 40 d) and Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) shows significant tumor growth inhibition.
| Animal Model: | Five-week-old male BALB/c nude mice with Panc-1 xenograft |
| Dosage: | 20 μM per kilogram |
| Administration: | Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) |
| Result: | The combination treatment showed significant tumor growth inhibition compared with other treatment groups (control 501±92 mg, Gemcitabine 294±46 mg, Clobenpropit 444±167 mg, and combination 154±54 mg). |
