Clobenpropit dihydrobromide

SKU: orb1298934

Description

Clobenpropit dihydrobromide is a potent histamine H3 receptor (H3R) antagonist and inverse agonist with a pEC50 of 8.07. This compound is widely used in neuroscience research to study H3R function in vitro and has been applied in vivo to explore its potential in models of cognitive disorders and sleep-wake regulation.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	145231-35-2
MW	470.7
Purity	99.86%
Formula	C₁₄H₁₉Br₂ClN₄S
SMILES	Br.Br.Clc1ccc(CNC(=N)SCCCc2cnc[nH]2)cc1
Target	Histamine Receptor,Apoptosis
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.12 mM);DMSO:4.71 mg/mL (10.01 mM)

Bioactivity

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Target IC50	H4 receptor:13 nM (Ki)\|H3LR (human):9.44 (pKi)\|H2 receptor:5.6 (pKi)\|H3LR (rat):9.75 (pKi)
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. Read more...
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. Read more...
Cell Research	Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1).Concentration: 50 Μm

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Clobenpropit, Clobenpropit dihydrobromide, Clobenpropit Dihydrobromide, agonist, cancer, antagonist, Apoptosis, inhibit, inverse, pancreatic, HistamineReceptor, Histamine Receptor, histamine H3R, Inhibitor, H3 receptor, H3LR

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Compound Identifiers

PubChem CID

11213569 ↗

Key Properties

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No computed properties available.

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