Tariquidar

Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (Kd = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine (Cay-11762) and paclitaxel (Cay-10461) in multidrug resistant CHrB30 cells, increasing the steady state accumulation to non-P-glycoprotein-expressing multidrug sensitive cell levels (EC50 = 487 nM). Tariquidar also enhances the distribution of its substrates, increasing the amount of substrate entering the CNS. When administered at doses of 2 and 6.25 mg/kg in mice in combination with the peripherally-restricted opioid loperamide, the latency to paw withdrawal in a hot plate assay increases, indicating that loperamide is transported into the CNS.Formal Name: N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarboxamide. CAS Number: 206873-63-4. Synonyms: XR9576. Molecular Formula: C38H38N4O6. Formula Weight: 646.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 2 mg/ml. lambdamax: 240 nm. SMILES: COC1=C(OC)C=C(CN(CCC2=CC=C(NC(C3=CC(OC)=C(OC)C=C3NC(C4=CN=C(C=CC=C5)C5=C4)=O)=O)C=C2)CC6)C6=C1. InChi Code: InChI=1S/C38H38N4O6/c1-45-33-18-25-14-16-42(23-28(25)19-34(33)46-2)15-13-24-9-11-29(12-10-24)40-38(44)30-20-35(47-3)36(48-4)21-32(30)41-37(43)27-17-26-7-5-6-8-31(26)39-22-27/h5-12,17-22H,13-16,23H2,1-4H3,(H,40,44)(H,41,43). InChi Key: LGGHDPFKSSRQNS-UHFFFAOYSA-N.