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Chemical Structure : HSK16149
Catalog No.: PC-49748Not For Human Use, Lab Use Only.
HSK16149 (HSK 16149) 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.
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HSK16149 (HSK 16149) 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.
| M.Wt | 209.29 | |
| Formula | C12H19NO2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xiaoli Gou , et al. J Pharmacol Exp Ther. 2021 Mar;376(3):330-337.
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