CFTR activator 1 

CFTR activator 1 is a potent and selective CFTR activator, with an EC₅₀ of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease^[1].

EC50: 23 nM (CFTR)^[1]

CFTR activator 1 (compound 16d) (30 nM-10 μM) potently activates CFTR chloride channel in FRT cells expressing human CFTR, with an EC₅₀ of 342 nM in the presence of 50 nM Forskolin^[1].
CFTR activator 1 (30 μM; pretreated for 10 min or 5 min) does not affect channel activities of ANO1 and VRAC in FRT cells expressing human ANO1 and in LN215 cells expressing a halide sensors YFP-F46L/H148Q/I152L^[1].
CFTR activator 1 (30 μM; 10 min) slightly increases cAMP level compared to the control in CHO-K1 cells^[1].
CFTR activator 1 (30 μM; 48 h) does not affect the cell viability of CorE and ConjE^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CFTR activator 1 (compound 16d) (2060 μM; 5 μL of eye drops; 3 times a day for 10 d) enhances tear secretion and improves corneal erosion in a mouse model of dry eye disease (DED). CFTR activator 1 reduces mRNA expression of pro-inflammatory cytokines including IL-1β, IL-17, and TNF-α and MMP2 in cornea and conjunctiva of DED mice^[1].
CFTR activator 1 (0.1 mg/eye; single topical instillation of eye drops) is well distributed in CFTR-expressing target tissues (cornea and conjunctiva) of male New Zealand White Rabbit, is maintained for a long period of time, and has a negligible systemic exposure^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

485.53

C₂₇H₂₇N₅O₄

2768261-09-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kim BY, et, al. Synthetic Strategies for Improving Solubility: Optimization of Novel Pyrazolo[1,5- a]pyrimidine CFTR Activator That Ameliorates Dry Eye Disease. J Med Chem. 2023 Jan 12;66(1):413-434.  [Content Brief]