Clobenpropit dihydrobromide - CAS:145231-35-2

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Clobenpropit dihydrobromide

目录号 : KM9483 CAS No. : 145231-35-2 纯度 : 98%

Data Sheet 产品使用指南

Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂，对组胺 H3LR 的 pEC₅₀ 为 8.07。Clobenpropit dihydrobromide 对组胺 H4 受体起部分激动剂的作用，K_i 为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (K_i 为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (K_i 为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apoptosis)。

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5mg		In-stock

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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. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.

体外研究

Clobenpropit binds to human H3LR and rat H3LR with pK_is of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pK_is of 5.2 and 5.6, respectively).
Clobenpropit inhibits [H]-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).
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC₅₀ 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).

分子式

C₁₄H₁₉Br₂ClN₄S

分子量

470.65

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.

纯度： 98%

Data Sheet

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