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

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 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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      Übersicht

      Replacement Information

      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
      Applications
      Biological Information
      Primary TargetMDR1
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      533794 0

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Laughney, A.M., et al. 2014. Sci. Trans. Med. 6, 261ra152.
      Kwak, J. O., et al. 2010. Eur. J. Pharm. 627, 92.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision16-March-2017 JSW
      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
      DescriptionA 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.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number849675-66-7
      Chemical formulaC₃₈H₃₆N₆O₇
      Purity≥97% by HPLC
      SolubilityDMSO (2 mg/ml)
      Storage Protect from light
      -20°C
      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.
      Toxicity Standard Handling
      ReferencesLaughney, A.M., et al. 2014. Sci. Trans. Med. 6, 261ra152.
      Kwak, J. O., et al. 2010. Eur. J. Pharm. 627, 92.