C3001a

C3001a is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2. 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).Formal Name: (1S,3R)-3-[[[4-(6-methyl-2-benzothiazolyl)phenyl]amino]carbonyl]-cyclopentanecarboxylic acid. CAS Number: 2415154-29-7. Molecular Formula: C21H20N2O3S. Formula Weight: 380.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.09 mg/ml. lambdamax: 215, 330 nm. SMILES: CC1=CC=C2N=C(SC2=C1)C3=CC=C(C=C3)NC([C@H]4C[C@@H](C(O)=O)CC4)=O. InChi Code: InChI=1S/C21H20N2O3S/c1-12-2-9-17-18(10-12)27-20(23-17)13-5-7-16(8-6-13)22-19(24)14-3-4-15(11-14)21(25)26/h2,5-10,14-15H,3-4,11H2,1H3,(H,22,24)(H,25,26)/t14-,15+/m1/s1. InChi Key: OUAZWUKQRHZQNC-CABCVRRESA-N.