145231-35-2
![145231-35-2 结构式](/CAS/GIF/145231-35-2.gif)
基本信息
氯苯丙替二氢溴酸盐
丙酸倍氯松二溴酸盐溶液,100PPM
丙酸倍氯松二溴酸盐溶液,1000PPM
Clobenpropit dihydrobromide Solution, 100ppm
Clobenpropit dihydrobromide Solution, 1000ppm
3-(1H-Imidazol-4-yl)propyl 4-Chlorobenzylcarbamimidothioate Dihydrobromide
Apoptosis,inhibit,Clobenpropit dihydrobromide,histamine H3R,antagonist,inverse,Inhibitor,pancreatic,agonist,cancer,H3LR,Histamine Receptor
物理化学性质
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/04/30 | C3446 | 氯苯丙替二氢溴酸盐 Clobenpropit Dihydrobromide | 145231-35-2 | 25mg | 905元 |
常见问题列表
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). |