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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
533794
  
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Overview

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
Catalogue Number GTIN
533794 0

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Laughney, A.M., et al. 2014. Sci. Trans. Med. 6, 261ra152.
Kwak, J. O., et al. 2010. Eur. J. Pharm. 627, 92.
Data Sheet

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.