Clobenpropit (dihydrobromide)

• CAS Number:

  145231-35-2

• 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 [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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

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

• Clinical Information:

  No Development Reported