丙酸倍氯松二溴酸盐溶液,1000PPM
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- CAS号:
- 145231-35-2
- 英文名:
- N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
- 英文别名:
- Clobenpropit (hydrobromide);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
- 中文名:
- 丙酸倍氯松二溴酸盐溶液,1000PPM
- 中文别名:
- 丙酸倍氯松二溴酸盐;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
- CBNumber:
- CB42463700
- 分子式:
- C14H17ClN4S.2BrH
- 分子量:
- 470.659
- MOL File:
- 145231-35-2.mol
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丙酸倍氯松二溴酸盐溶液,1000PPM化学性质
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熔点:
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205°C(lit.)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml
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形态:
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powder to crystal
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颜色:
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White to Gray to Red
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水溶解性:
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Soluble to 100 mM in water
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丙酸倍氯松二溴酸盐溶液,1000PPM性质、用途与生产工艺
Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂，对组胺 H3LR 的 pEC 50 为 8.07。Clobenpropit dihydrobromide 对组胺 H4 受体起部分激动剂的作用，Ki 为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (Ki 为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (Ki 为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apoptosis)。
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Human H3LR
9.44 (pKi)
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Rat H3LR
9.75 (pKi)
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H
4
receptor
13 nM (Ki)
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H
2
Receptor
5.6 (pKi)
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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
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Cell Line:
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Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1)
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Concentration:
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50 μM
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Incubation Time:
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Result:
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Enhanced apoptotic cell death in combination of Gemcitabine (5 μM).
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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.
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Animal Model:
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Five-week-old male BALB/c nude mice with Panc-1 xenograft
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Dosage:
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20 μM per kilogram
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Administration:
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Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d)
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Result:
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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).
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丙酸倍氯松二溴酸盐溶液,1000PPM
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
145231-35-2, 丙酸倍氯松二溴酸盐溶液,1000PPM 相关搜索:
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- Apoptosis,inhibit,Clobenpropit dihydrobromide,histamine H3R,antagonist,inverse,Inhibitor,pancreatic,agonist,cancer,H3LR,Histamine Receptor
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