Clobenpropit dihydrobromide

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Clobenpropit dihydrobromide 

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)。

Clobenpropit dihydrobromide

Clobenpropit dihydrobromide Chemical Structure

CAS No. : 145231-35-2

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生物活性

Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR[1]. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM)[2]. Clobenpropit dihydrobromide increases apoptosis[3].

IC50 & Target[1][2]

Human H3LR

9.44 (pKi)

Rat H3LR

9.75 (pKi)

H4 receptor

13 nM (Ki)

H2 Receptor

5.6 (pKi)

体外研究
(In Vitro)

Clobenpropit binds to human H3LR and rat H3LR with pKis of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pKis of 5.2 and 5.6, respectively)[1].
Clobenpropit inhibits [3H]-dopamine transport by SH-SY5Y cells in a concentration dependent manner with maximum inhibition 82.7±2.8 % and IC50 490 nM (pIC50 6.31±0.11)[2].
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC50 1 μM for the NR1/NR2B receptor)[2].
Clobenpropit (50 μM) and Gemcitabine (5 μM) combination therapy significantly increases apoptosis of Panc-1, MiaPCa-2 and AsPC-1 compared with control[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[3]

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
(In Vivo)

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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old male BALB/c nude mice with Panc-1 xenograft[3]
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).

分子量

470.65

Formula

C14H19Br2ClN4S
CAS 号

145231-35-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Esbenshade TA, et al. Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96.

    [2]. Mena-Avila E, et al. Clobenpropit, a histamine H3 receptor antagonist/inverse agonist, inhibits [3H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes. Pharmacol Rep. 2018 Feb;70(1):146-155.

    [3]. Paik WH, et al. Clobenpropit enhances anti-tumor effect of gemcitabine in pancreatic cancer. World J Gastroenterol. 2014 Jul 14;20(26):8545-57.

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