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CR4056

Chemical Structure : CR4056

CAS No.: 1004997-71-0

CR4056 (CR 4056;CR-4056)

Catalog No.: PC-35650Not For Human Use, Lab Use Only.

CR4056 (CR 4056, CR-4056) is a novel, orally active imidazoline-2 receptor (I2R) ligand with binding IC50 of 596 nM, also selectively inhibits the enzymatic activity of MAO-A with IC50 of 202.7 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CR4056 (CR 4056, CR-4056) is a novel, orally active imidazoline-2 receptor (I2R) ligand with binding IC50 of 596 nM, also selectively inhibits the enzymatic activity of MAO-A with IC50 of 202.7 nM; increases norepinephrine (NE) tissue levels both in the rat cerebral cortex and lumbar spinal cord, shows ED50 of 5.8 mg/kg in CFA rat model of inflammatory pain; shows high effectivity against bortezomib-induced painful neuropathy in rats.

Pain

Phase 2 Clinical

Physicochemical Properties

M.Wt 272.311
Formula C17H12N4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(1H-imidazol-1-yl)-2-phenylquinazoline

References

1. Ferrari F, et al. J Pain Res. 2011;4:111-25.

2. Thorn DA, et al. Br J Pharmacol. 2012 Jul;166(6):1936-45.

3. Meregalli C, et al. J Pain Res. 2012;5:151-67.

4. Lanza M, et al. Br J Pharmacol. 2014 Aug;171(15):3693-701.

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