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Clobenpropit (dihydrobromide)
SKU
HY-101198-10 mg
Category Reference compound
Tags Apoptosis;GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling, Apoptosis;Histamine Receptor, Cancer; Neurological Disease
$110 – $1,200
Products Details
Product 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].
Web ID
– HY-101198
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C14H19Br2ClN4S
References
– [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.
CAS Number
– 145231-35-2
Molecular Weight
– 470.65
Compound Purity
– 98.99
SMILES
– N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br
Clinical Information
– No Development Reported
Research Area
– Cancer; Neurological Disease
Solubility
– DMSO : 125 mg/mL (ultrasonic)
Target
– Apoptosis;Histamine Receptor
Isoform
– H1 Receptor;H2 Receptor;H3 Receptor;H4 Receptor
Pathway
– Apoptosis;GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling
Product type
– Reference compound
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