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505985 CFTR Activator, Cact-A1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₃N₅O

Products

Catalog NumberPackaging Qty/Pack
5.05985.0001 Glass bottle 10 mg
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®
Synonyms5-((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, Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1
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
Global Trade Item Number
Catalog Number GTIN
5.05985.0001 04055977262575

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
Synonyms5-((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, Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1
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 Protect from light
+2°C to +8°C
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.