KCL-286

KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM) . KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM) . KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury[1][3].

Product Specifications

CAS Number

[1952276-71-9]

Product Name Alternative

C286

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

RAR/RXR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Inflammation/Immunology; Neurological Disease; Others

Assay Protocol

https://www.medchemexpress.com/anticancer-agent-168.html

Purity

98.93

Solubility

DMSO : 6.25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=CC=C(C)C2=C1OC(C3=NC(C4=CC=C(C(O)=O)C=C4)=NO3)=C2

Molecular Formula

C19H14N2O4

Molecular Weight

334.33

Precautions

H302, H312, H332

References & Citations

[1]Goncalves MB, et al. Phase 1 safety, tolerability, pharmacokinetics and pharmacodynamic results of KCL-286, a novel retinoic acid receptor-β agonist for treatment of spinal cord injury, in male healthy participants. Br J Clin Pharmacol. 2023 Jul 15..|[2]Goncalves, M. B., (2024) . C286, an orally available retinoic acid receptor β agonist drug, regulates multiple pathways to achieve spinal cord injury repair. Frontiers in molecular neuroscience, 17, 1411384. |[3]Borthwick, A. D., et al., (2020) . Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review. Bioorganic & medicinal chemistry, 28 (20), 115664.