505985 CFTR Activator, Cact-A1 - Calbiochem

505985
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₃N₅O

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, non-toxic aminopyrazolocarbonitrile compound that acts as a potent, selective, reversible and cAMP-independent activator of CFTR-dependent Cl- channel in airway epithelial cells (EC50 = 1.6 µM in CFTR-expressing Fisher rat thyroid cells). Also shown to activate ΔF508-CFTR in primary CF-HBE cell cultures (EC50 = 3.5 µM). Reported to directly bind to the same site as CFTRinh-172 (Cat. No. 219670, Cat. No. 219674). Does neither elevate intracellular cAMP levels nor appear to have any requirement for cAMP agonist, such as forskolin (Cat. No. 344270, Cat. No. 344282). Shown to additively potentiate the G551D-CFTR Cl- current activated by forskolin with CFTR potentiator, VX-770. Exerts no effect on either Ca2+-activated Cl- channel (TMEM16A) or intracellular Ca2+ levels.
      Catalogue Number505985
      Brand Family Calbiochem®
      SynonymsCystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1, 5-((Z)-2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-3-amino-1H-pyrazole-4-carbonitrile, (Z)-3-(2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-5-amino-1H-pyrazole-4-carbonitrile
      References
      ReferencesNamkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      Product Information
      FormLight yellow powder
      Hill FormulaC₁₆H₁₃N₅O
      Chemical formulaC₁₆H₁₃N₅O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCFTR
      Purity≥98% 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 Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CFTR Activator, Cact-A1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      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.

      Revision18-October-2013 JSW
      SynonymsCystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1, 5-((Z)-2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-3-amino-1H-pyrazole-4-carbonitrile, (Z)-3-(2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-5-amino-1H-pyrazole-4-carbonitrile
      DescriptionA non-cytotoxic (30 µM for 48 h in human airway epithelial Calu-3 cultures) aminopyrazolocarbonitrile compound that is shown to activate both wt- and ΔF508-CFTR channel activity in a cAMP-independent, reversible, and CFTRinh-172- (Cat. Nos. 219670 & 219674) blockable (IC50 & IC100 = 0.37 & 30 µM, respectively, against 30 µM Cact using Fisher rat thyroid/FRT cells with wt-CFTR) manner, without affecting CaCC (Calcium-activated chloride channel) function or cellular levels of Ca2+ and cAMP. The maximum activation inducible by Cact-A1 (ECmax = 13 to 30 µM in Cl- current induction using in Fisher rat thyroid/FRT and primary human bronchial epithelial/HBE cells) is comparable to that achievable via cAMP stimulation by Forskolin treatment (ECmax = 20 µM; Cat. Nos. 344270 & 34427082), which cannot be further enhanced by Forskolin co-treatment in cells expressing wt-CFTR, although additive effects are seen when Cact-A1 and Forskoklin are applied at suboptimal concentrations to cells with wt-CFTR or when the two drugs are applied at respective ECmax to cells with surface ΔF508-CFTR. Neither Cact-A1 nor Forskolin alone (at 30 µM; and 20 µM;, respectively) can effectively activate FRT with surface G551D-CFTR or primary HNPE (human nasal polyp epithelial) cells with surface G551D/Y1092X-CFTR, while Cact-A1-Forskolin co-treatment results in synergistic activation and maximally achievable activation is reported with a three-drug co-treatment using Cact-A1, Forskolin, and VX-770 (at 30, 20, and 10 µM, respectively).
      FormLight yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₃N₅O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesNamkung, W., et al. 2013. Mol. Pharmacol. 84, 384.