TCS 1102

Orexin receptors 1 (OX1R) and OX2R mediate the action of the neuropeptides orexin A and orexin B. TCS 1102 is a dual antagonist of both OX1R and OX2R (Kis = 0.2 and 3 nM, respectively). It is a poor substrate for P-glycoprotein and, as a result, demonstrates good brain penetration when administered intraperitoneally. Dual orexin receptor antagonists, including TCS 1102, promote sleep and prevent drug-induced plasticity and drug relapse. Systemic injection of TCS 1102 (10 mg/kg i.p.) in rats decreases fear and anxiety in response to acute episodes of stress.Formal Name: (2S)-N-[1,1'-biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide. CAS Number: 916141-36-1. Molecular Formula: C27H26N4O2S. Formula Weight: 470.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7) (1:10): 0.09 mg/ml, DMSO: 14 mg/ml, Ethanol: 10 mg/ml. lambdamax: 205, 284, 291 nm. SMILES: O=C(N1[C@@H](C(NC2=C(C3=CC=CC=C3)C=CC=C2)=O)CCC1)CSC4=NC5=CC=CC=C5N4C. InChi Code: InChI=1S/C27H26N4O2S/c1-30-23-15-8-7-14-22(23)29-27(30)34-18-25(32)31-17-9-16-24(31)26(33)28-21-13-6-5-12-20(21)19-10-3-2-4-11-19/h2-8,10-15,24H,9,16-18H2,1H3,(H,28,33)/t24-/m1/s1. InChi Key: YSBGRVXJEMSEQY-XMMPIXPASA-N.