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Clobenpropit dihydrobromide

Catalog No. T8439   CAS 145231-35-2

Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)

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Clobenpropit dihydrobromide Chemical Structure
Clobenpropit dihydrobromide, CAS 145231-35-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 38.00
5 mg In stock $ 89.00
10 mg In stock $ 155.00
25 mg In stock $ 347.00
50 mg In stock $ 587.00
100 mg In stock $ 839.00
1 mL * 10 mM (in DMSO) In stock $ 108.00
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Purity: 99.48%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)
Targets&IC50 H2 receptor:5.6 (pKi), Human H3LR:9.44 (pKi), H4 receptor:13 nM (Ki), Rat H3LR:9.75 (pKi)
In vitro Clobenpropit inhibited cell migration and increased apoptosis of pancreatic cancer cells in combination with gemcitabine.?Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction[1].
In vivo Clobenpropit inhibited tumor growth (gemcitabine 294 46 mg vs combination 154 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse.
Cell Research Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1).Concentration: 50 Μm
Molecular Weight 470.7
Formula C14H19Br2ClN4S
CAS No. 145231-35-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.71 mg/mL (10 mM), Sonification is recommended

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Histamine & Melatonin Receptor-Targeted Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Inhibitor Library GPCR Compound Library Apoptosis Compound Library Neurotransmitter Receptor Compound Library Anti-Parkinson's Disease Compound Library Bioactive Compound Library

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Keywords

Clobenpropit dihydrobromide 145231-35-2 Apoptosis GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor inhibit Clobenpropit histamine H3R antagonist inverse Inhibitor pancreatic agonist cancer H3LR Clobenpropit Dihydrobromide inhibitor

 

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