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R481
- Development stage
- Preclinical
- Lead developer
- Rigel Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intperitoneal
01
Overview
R481 is a brain-permeable, small molecule AMP-activated protein kinase (AMPK) activator developed by Rigel Pharmaceuticals. It acts as an indirect, metformin-like AMPK activator via mitochondrial complex I inhibition, exhibiting high potency and a positive brain-to-plasma distribution. R481 is being investigated for its potential to prevent hypoglycemia and improve glucose counterregulation in patients with diabetes, particularly Type 1 and advanced insulin-treated Type 2 diabetes. By activating central AMPK in the hypothalamus, R481 stimulates the autonomic nervous system to augment the glucagon response to low blood sugar levels without worsening fasting hyperglycemia or altering insulin sensitivity.
02
Targets
ND1 (Mitochondrial electron transport chain complex I)
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