TD-4208

TD-4208 is an antagonist of muscarinic acetylcholine receptors (mAChRs, Kis = 0.42, 0.3, 0.18, and 0.55 nM for M1, M2, M3, and M4 receptors, respectively, in membranes from CHO-K1 cells expressing the human receptors). It is selective for these receptors over M5 muscarinic receptors (Ki = 6.31 nM in membranes from CHO-K1 cells expressing the human receptor). TD-4208 inhibits calcium mobilization induced by acetylcholine (AChE, Cay-23829) in CHO-K1 cells expressing M2 and M3 muscarinic receptors. It decreases AChE-induced contractions in isolated rat trachea in a concentration-dependent manner. TD-4208 decreases AChE-induced bronchoconstriction and reduces salivation induced by pilocarpine, a surrogate test for noisy breathing, in rats (ID50s = 45 and 1,164 µg/ml, respectively). It also decreases AChE-induced bronchoconstriction in dogs when administered intranasally at doses of 10 and 30 µg/kg. Formulations containing TD-4208 have been used in the treatment of chronic obstructive pulmonary disease (COPD).Formal Name: N-[1,1'-biphenyl]-2-yl-carbamic acid, 1-[2-[[4-[[4-(aminocarbonyl)-1-piperidinyl]methyl]benzoyl]methylamino]ethyl]-4-piperidinyl ester. CAS Number: 864750-70-9. Synonyms: Revefenacin. Molecular Formula: C35H43N5O4. Formula Weight: 597.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, Ethanol: 25 mg/ml. SMILES: O=C(NC1=C(C2=CC=CC=C2)C=CC=C1)OC3CCN(CC3)CCN(C)C(C4=CC=C(CN5CCC(CC5)C(N)=O)C=C4)=O. InChi Code: InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)23-24-39-21-17-30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28,30H,15-25H2,1H3,(H2,36,41)(H,37,43). InChi Key: FYDWDCIFZSGNBU-UHFFFAOYSA-N.