TS-011

TS-011 is an inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. It inhibits 20-HETE synthesis in human and rat renal microsomes (IC50s = 8.42 and 9.19 nM, respectively), as well as by the cytochrome P450 (CYP) isoforms CYP4F2, CYP4F3A, CYP4F3B, and CYP4A11 in cell-free assays (IC50s = 30.4, 42.6, 43.0, and 188 nM, respectively). It is selective for these CYPs over CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >60 µM for all), as well as a panel of receptors and other enzymes at 1 µM. TS-011 (0.01-1 mg/kg, i.v.) reverses decreases in cerebral blood flow and increases in cerebrospinal fluid 20-HETE levels in a rat model of subarachnoid hemorrhage. It also reduces infarct volume and prevents neurological deficits in a rat model of stroke induced by middle cerebral artery occlusion (MCAO).Formal Name: N-[3-chloro-4-(4-morpholinyl)phenyl]-N'-hydroxy-methanimidamide. CAS Number: 339071-18-0. Molecular Formula: C11H14ClN3O2. Formula Weight: 255.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3 mg/ml, DMSO: 2 mg/ml, Ethanol: insol, PBS (pH 7.2): insol. lambdamax: 213, 271 nm. SMILES: ClC1=CC(N=CNO)=CC=C1N2CCOCC2. InChi Code: InChI=1S/C11H14ClN3O2/c12-10-7-9(13-8-14-16)1-2-11(10)15-3-5-17-6-4-15/h1-2,7-8,16H,3-6H2,(H,13,14). InChi Key: ZTXADXBIGLLOFX-UHFFFAOYSA-N.