A P-gp inhibitor; binds to P-glycoprotein (Kd = 5.1 nM); inhibits transport of vinblastine and paclitaxel in CHrB30 cells

Tariquidar – 100 mg

Brand:
Cayman
CAS:
206873-63-4
Storage:
-20
UN-No:
Non-Hazardous - /

Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (Kd = 5.1 nM) and inhibits transport activity.{41596} It inhibits transport of vinblastine (Item No. 11762) and paclitaxel (Item No. 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.{41597} 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.  

 

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SKU: 24180 - 100 mg Category:

Description

A P-gp inhibitor; binds to P-glycoprotein (Kd = 5.1 nM); inhibits transport of vinblastine and paclitaxel in CHrB30 cells, leading to accumulation to control levels (EC50 = 487 nM); increases the amount of its substrate that enters 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

Synonyms:  XR9576

Molecular weight: 646.7

CAS: 206873-63-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Multidrug Resistance||Research Area|Neuroscience|Pain Research

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