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Clobenpropit (dihydrobromide)

Product Specifications

UNSPSC Description

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].

Target Antigen

Apoptosis; Histamine Receptor

Type

Reference compound

Related Pathways

Apoptosis;GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/clobenpropit-dihydrobromide.html

Purity

98.99

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br

Molecular Weight

470.65

References & Citations

[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 [<sup>3</sup>H]-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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-101198/Clobenpropit-dihydrobromide-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-101198/Clobenpropit-dihydrobromide-SDS-MedChemExpress.pdf

Clinical Information

No Development Reported

CAS Number

145231-35-2

Available Sizes

Curated Selection

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