505985 CFTR Activator, Cact-A1 - Calbiochem

505985
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₃N₅O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05985.0001
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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
          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

          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.