1952276-71-9
Chemical Structure
KCL-286
Synonym(s): C286
- CAS No.: 1952276-71-9
- Formula:C19H14N2O4
- Molecular Weight:334.33
IUPAC Name: 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid
InChIKey: AVCXUODHLRZJJP-UHFFFAOYSA-N
SMILES: CC1=CC=C(C)C2=C1OC(C3=NC(C4=CC=C(C(O)=O)C=C4)=NO3)=C2
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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KCL-286 | 98.93% | 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. | ||||||||||||||||||||
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- [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.. [Content Brief]
- [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. [Content Brief]
Keywords
