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533794 MDR1 Inhibitor, HM30181 - CAS 849675-66-7 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(2-(2-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)-4-oxo-4H-chromene-2-carboxamide, MDR1 ATPAse inhibitor, HM30181, ABAC1 Inhibitor, HM30181, P-gp Inhibitor, HM30181

Primary Target: MDR1
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      Overview

      Key Spec Table

      CAS #Empirical Formula
      849675-66-7C₃₈H₃₆N₆O₇
      Description
      Overview

      This product has been discontinued.



      A cell-permeable chromene-2-carboxamide compound that acts as a selective and highly potent inhibitor of the ATPase activity of multi-drug resistance protein 1 (MDR1, ABAC1, IC50 = 630 pM). Does not affect MRP1, MRP2, MRP3, and has only a weak effect on BCRP (ABCG2) at higher concentrations. Shown to block trans-epithelial transport of paclitaxel in Madin-Darby canine kidney cells (MDCK; IC50 = 35.5 nM). When co-administered (at 10 mg/kg, p.o.), it enhances the oral bioavailability of paclitaxel by about 12-fold and suppresses the growth of HT-29 tumor xenografts in nude mice (with 20 mg/kg paclitaxel, p.o.). Also shown to improve pharmacokinetic profile of paclitaxel (Cmax = 1253 vs 127 ng/ml) without altering its half-life.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533794
      Brand Family Calbiochem®
      SynonymsN-(2-(2-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)-4-oxo-4H-chromene-2-carboxamide, MDR1 ATPAse inhibitor, HM30181, ABAC1 Inhibitor, HM30181, P-gp Inhibitor, HM30181
      References
      ReferencesLaughney, A.M., et al. 2014. Sci. Trans. Med. 6, 261ra152.
      Kwak, J. O., et al. 2010. Eur. J. Pharm. 627, 92.
      Product Information
      CAS number849675-66-7
      FormYellow solid
      Hill FormulaC₃₈H₃₆N₆O₇
      Chemical formulaC₃₈H₃₆N₆O₇
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetMDR1
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      533794 0