产品
编 号：F755864
分子式：C27H27N5O4
分子量：485.53
分子式：C27H27N5O4
分子量：485.53
产品类型
规格
价格
是否有货
结构图
CAS No: 2768261-09-0
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Eight weeks old female C57BL/6J mice were injected Scopolamine hydrobromide
Dosage:2060 μM, 5 μL, and maintained for 30 s
Administration:Eye drop application was done in both eyes, three times a day (11:00 am, 2:00 pm, 5:00 pm) for 10 days
Result:Enhanced tear secretion and improved corneal erosion.Reduced mRNA expression of pro-inflammatory cytokines including IL-1β, IL-17, and TNF-α and MMP2 in cornea and conjunctiva.
体外研究：
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.
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.
体内研究：
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.Animal Model:Eight weeks old female C57BL/6J mice were injected Scopolamine hydrobromide
Dosage:2060 μM, 5 μL, and maintained for 30 s
Administration:Eye drop application was done in both eyes, three times a day (11:00 am, 2:00 pm, 5:00 pm) for 10 days
Result:Enhanced tear secretion and improved corneal erosion.Reduced mRNA expression of pro-inflammatory cytokines including IL-1β, IL-17, and TNF-α and MMP2 in cornea and conjunctiva.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备