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]. IC50 & Target:RAR α (EC₅₀ = 26 nM);RAR β (EC₅₀ = 1.9 nM);RAR γ (EC₅₀ = 11 nM)^[1] In Vitro:KCL-286 (0.1 μM, 72 h) increases the neurite density and the number of synapses to a significant extent which activates RARβ2^[2]. In Vivo:KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) modulates various regenerative pathways as well as restoring ECM levels and cell adhesion molecules in the injured rat model^[2].
KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) improves the hind limb locomotor function in moderate thoracic SC contusion rat model^[2].
KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) achieves full locomotor and sensory recovery after 3 weeks in C5-T1 dorsal root avulsion rat model^[2].