KCL-286

• Description :

  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 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [1952276-71-9]