丙酸倍氯松二溴酸盐
- CAS号:145231-35-2
- 英文名:N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
- 中文名:丙酸倍氯松二溴酸盐
- CBNumber:CB42463700
- 分子式:C14H17ClN4S.2BrH
- 分子量:470.659
- MOL File:145231-35-2.mol
- 熔点 :205°C(lit.)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml
- 形态 :powder to crystal
- 颜色 :White to Gray to Red
- 水溶解性 :Soluble to 100 mM in water
- 海关编码 :2933.29.4300
丙酸倍氯松二溴酸盐性质、用途与生产工艺
- 生物活性 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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靶点
Human H3LR
9.44 (pKi)
Rat H3LR
9.75 (pKi)
H 4 receptor
13 nM (Ki)
H 2 Receptor
5.6 (pKi)
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体外研究
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). -
体内研究
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).
- 更新日期：2024/11/08
- 产品编号：C3446
- 产品名称：氯苯丙替二氢溴酸盐 Clobenpropit Dihydrobromide
- CAS编号：145231-35-2
- 包装：25mg
- 价格：905元
- 公司名称：TCI AMERICA
- 联系电话：800-4238616
- 电子邮件：sales@tciamerica.com
- 国家：美洲
- 产品数：23653
- 优势度：75
