Catalog No.: PC-49748Not For Human Use, Lab Use Only.
HSK16149 (Crisugabalin) is a potent selective ligand of voltage-gated calcium channel (VGCC) α2δ subunit with IC50 of 3.96 nM in competitive [3H]gabapentin binding assays.
HSK16149 (Crisugabalin) is a potent selective ligand of voltage-gated calcium channel (VGCC) α2δ subunit with IC50 of 3.96 nM in competitive [3H]gabapentin binding assays.
HSK16149 exhibited stronger (>20-fold) affinity than pregabalin.
In rat models of neuropathic pain, the minimum effective dose (MED) of HSK16149 was 10 mg/kg, and the efficacy was similar to that of 30 mg/kg pregabalin.
HSK16149 could persist up to 24 hours postadministration at 30 mg/kg, whereas the efficacy of pregabalin lasted only for 12 hours at 30 mg/kg in streptozotocin-induced diabetic neuropathy model.
HSK16149 also inhibit mechanical allodynia in intermittent cold stress model and decrease phase II pain behaviors in formalin-induced nociception model.
