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CFTR activator 1

CAS No. : 2768261-09-0

MCE 站：CFTR activator 1

产品活性：CFTR activator 1 是一种有效和选择性的 CFTR 激活剂，EC₅₀ 值为 23 nM。CFTR activator 1 可用于改善干眼症。

研究领域：Membrane Transporter/Ion Channel

作用靶点：CFTR

In Vitro: 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.
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.
CFTR activator 1 (30 μM; 10 min) slightly increases cAMP level compared to the control in CHO-K1 cells.
CFTR activator 1 (30 μM; 48 h) does not affect the cell viability of CorE ａnd ConjE.

In Vivo: 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.
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.

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