1. Membrane Transporter/Ion Channel
  2. CFTR
  3. 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.

For research use only. We do not sell to patients.

CFTR activator 1 Chemical Structure

CFTR activator 1 Chemical Structure

CAS No. : 2768261-09-0

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

EC50: 23 nM (CFTR)[1]

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[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].

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

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[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].

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

Animal Model: Eight weeks old female C57BL/6J mice were injected Scopolamine hydrobromide[1]
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.
Molecular Weight

485.53

Formula

C27H27N5O4

CAS No.
SMILES

O=C(N1C[C@@H](N(CC1)C(C2=CC=CC=C2)=O)C)C3=NN4C(C5=CC(OC)=C(C=C5)OC)=CC=NC4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CFTR activator 1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CFTR activator 1
Cat. No.:
HY-152264
Quantity:
MCE Japan Authorized Agent: