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CR4056

Catalog No. T15010   CAS 1004997-71-0
Synonyms: 6-(1H-imidazol-1-yl)-2-phenylquinazoline

CR4056 (6-(1H-imidazol-1-yl)-2-phenylquinazoline) is a selective inhibitor of MAO-A with IC50 of 202.7 nM and a ligand of I2-imidazoline receptor with IC50 of 596 nM.

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CR4056 Chemical Structure
CR4056, CAS 1004997-71-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 195.00
5 mg In stock $ 437.00
10 mg In stock $ 646.00
25 mg In stock $ 987.00
50 mg In stock $ 1,380.00
100 mg In stock $ 1,860.00
500 mg In stock $ 3,720.00
1 mL * 10 mM (in DMSO) In stock $ 446.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CR4056 (6-(1H-imidazol-1-yl)-2-phenylquinazoline) is a selective inhibitor of MAO-A with IC50 of 202.7 nM and a ligand of I2-imidazoline receptor with IC50 of 596 nM.
Targets&IC50 MAO-A:202.7 nM, I2R:596 nM
In vitro The co-treatment of CR4056 (3-30 μM) with Bortezomib does not induce any significant difference in cell survival compared with BTZ-treated cells, either in H929 or in RPMI 8226 myeloma cells[1].
In vivo CR4056 (30 mg/kg) completely reverses the effect of capsaicin, increasing the paw withdrawal threshold (PWT) to 239. CR4056 obviously increases the mechanical withdrawal thresholds of both ipsilateral (F[4, 30]=19.97) and contralateral (F[4, 30]=31.58) hind paws. CR4056 dose-dependently reduces mechanical hyperalgesia with ED50 of 5.8 mg/kg. CR4056 dose-dependently decreases streptozotocin (STZ)-induced diabetic pain in rats (F[4, 35]=31.27). CR4056 (20 mg/kg; oral) increases endogenous norepinephrine (NE) levels by 68.2% in the parieto-occipital cortex. CR4056 (20 mg/kg; p.o.) obviously increases NE levels both in the cerebral cortex (63.1%) and in the lumbar spinal cord (51.3%). CR4056 (10 mg/kg) and Piroxicam (10 mg/kg) obviously reverse the decrease in the withdrawal threshold caused by Capsaicin[2].
Synonyms 6-(1H-imidazol-1-yl)-2-phenylquinazoline
Molecular Weight 272.3
Formula C17H12N4
CAS No. 1004997-71-0

Storage

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

Solubility Information

DMSO: 25 mg/mL (91.81 mM), Sonification is recommended.

H2O: < 0.1 mg/mL (insoluble)

TargetMolReferences and Literature

1. Meregalli C, et al. CR4056, a new analgesic I2 ligand, is highly effective against bortezomib-induced painful neuropathy in rats. J Pain Res. 2012;5:151-67. 2. Ferrari F, et al. Analgesic efficacy of CR4056, a novel imidazoline-2 receptor ligand, in rat models of inflammatory and neuropathic pain. J Pain Res. 2011;4:111-25.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library ReFRAME Related Library Mitochondria-Targeted Compound Library

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1-Methyl-2-undecyl-4(1H)-quinolone Vafidemstat (±)-Amiflamine PSB-1434 5-Hydroxy-1-methoxyxanthone RN-1 dihydrochloride Osthenol 7-Hydroxy-3,4-dihydro-2(1H)-quinolinone

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Keywords

CR4056 1004997-71-0 Metabolism Neuroscience MAO Imidazoline Receptor 6-(1H-imidazol-1-yl)-2-phenylquinazoline CR 4056 CR-4056 inhibitor inhibit

 

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