145231-35-2

中文名称丙酸倍氯松二溴酸盐溶液,1000PPM

英文名称 N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA

CAS 145231-35-2

分子式 C14H17ClN4S.2BrH

分子量 470.659

MOL 文件 145231-35-2.mol

更新日期 2023/09/15 22:54:22

145231-35-2 结构式

基本信息物理化学性质安全数据图谱信息丙酸倍氯松二溴酸盐溶液,1000PPM价格(试剂级) 常见问题列表

基本信息

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

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

物理化学性质

熔点205°C(lit.)

储存条件-20°C储存

溶解度DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml

形态粉末晶体

颜色白色到灰色到红色

水溶解性溶于水至100mM

安全数据

海关编码2933.29.4300

图谱信息

丙酸倍氯松二溴酸盐溶液,1000PPM(145231-35-2)核磁图(¹HNMR)

丙酸倍氯松二溴酸盐溶液,1000PPM价格(试剂级)

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

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)。

靶点

Human H3LR

9.44 (pKi)

Rat H3LR

9.75 (pKi)

H ₄ receptor

13 nM (Ki)

H ₂ Receptor

5.6 (pKi)

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).