C3001a is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2.{59302} It increases current amplitude in HEK293T cells expressing K2P2.1/TREK1 or K2P10.1/TREK2 (EC50s = 12.81 and 11.31 µM, respectively, for the human channels). C3001a is selective for K2P2.1/TREK1 and K2P10.1/TREK2 over a panel of five additional K2P channels at 10 µM. In vivo, C3001a (10 mg/kg) reduces edema and pancreatic necrosis in a mouse model of acute pancreatitis. It reduces mechanical and thermal hyperalgesia in a mouse model of chronic inflammatory pain induced by complete Freund’s adjuvant (CFA). C3001a (5 mg/kg) also reduces cold hyperalgesia in a mouse model of neuropathic pain induced by spared nerve injury (SNI).
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 2415154-29-7 |
| Molecular formula | C21H20N2O3S |
| Smiles | CC1=CC=C2N=C(SC2=C1)C3=CC=C(C=C3)NC([C@H]4C[C@@H](C(O)=O)CC4)=O |
| Molecular weight | 380,5 |
| Custom code | 2934.20 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
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