Tariquidar | 2853

Tariquidar is a potent, specific, noncompetitive inhibitor of P-glycoprotein (P-gp) (Kd = 5.1 nM). Tariquidar inhibits the ATPase activity of P-gp, suggesting that the modulating effect is derived from the inhibition of substrate binding, inhibition of ATP hydrolysis or both. At low concentrations, Tariquidar acts selectively as an inhibitor of P-gp and as a substrate of BCRP (breast cancer resistance protein). At much higher concentrations (≥100 nM). Tariquidar acts as an inhibitor of both P-gp and BCRP.

Tariquidar is a potent, specific, noncompetitive inhibitor of P-glycoprotein (P-gp) (Kd = 5.1 nM). Tariquidar inhibits the ATPase activity of P-gp, suggesting that the modulating effect is derived from the inhibition of substrate binding, inhibition of ATP hydrolysis or both. At low concentrations, Tariquidar acts selectively as an inhibitor of P-gp and as a substrate of BCRP (breast cancer resistance protein). At much higher concentrations (≥100 nM). Tariquidar acts as an inhibitor of both P-gp and BCRP.

2853 | Tariquidar DataSheet

Alternate Name/Synonyms: N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide; XR9576, XR 9576, XR-9576,Tariquidar

Appearance: Light yellow solid

Formulation: N/A

CAS Number: 206873-63-4

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₃₈H₃₈N₄O₆

Molecular Weight: 646.73

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (>6 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A P-glycoprotein (P-gp) inhibitor

MDL Number: N/A

PubChem CID: 148201

SMILES: COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC

InChi: 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