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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