2. Membrane Transporter/Ion Channel
  3. CFTR
  4. VRT-325

VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and P-gp. VRT-325 promotes maturation of CFTR and P-gp processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis[1][3].

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

VRT-325

VRT-325 Chemical Structure

CAS No. : 815592-21-3

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Based on 1 publication(s) in Google Scholar

VRT-325 Related Antibodies

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Description

VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and P-gp. VRT-325 promotes maturation of CFTR and P-gp processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis[1][2][3].

In Vitro

VRT-325 (30 min) directly interacts with I340C(TM6)/S877C(TM7) Cys-less/V510A CFTR in HEK 293 cells[1].
VRT-325 (5 µM; 24 h) partially rescues mature ΔF508-CFTR protein expression in CFBE-ΔF508 cells[2].
VRT-325 (5 µM; 24 h) rescues ΔF508-CFTR channel function in CFBE-ΔF508 cells[2].
VRT-325 (10 µM; 24 h) rescues ΔF508-CFTR channel function in primary human cystic fibrosis airway epithelial cells[2].
VRT-325 corrects Delta F508-CFTR misfolding and trafficking with an EC50 of approximately 2 μM[3].

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

VRT-325 Related Antibodies

Western Blot Analysis[2]

Cell Line: CFBE-ΔF508 cystic fibrosis airway epithelial cells
Concentration: 5 µM
Incubation Time: 24 h
Result: Increased mature CFTR band C expression to ~350% of the lysogeny broth (LB) control level.
Reduced mature CFTR band C expression to ~20% of the LB control level when combined with PsaDM, representing a significant decrease compared to VRT-325 treatment alone.
Molecular Weight

510.65

Formula

C27H34N4O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N1CCN(CC1)S(=O)(C2=CC=C(C=C2)OC)=O)C3=NC(OC4CCCCC4)=C5C=CC=CC5=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 45 mg/mL (88.12 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9583 mL 9.7914 mL 19.5829 mL
5 mM 0.3917 mL 1.9583 mL 3.9166 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9583 mL 9.7914 mL 19.5829 mL 48.9572 mL
5 mM 0.3917 mL 1.9583 mL 3.9166 mL 9.7914 mL
10 mM 0.1958 mL 0.9791 mL 1.9583 mL 4.8957 mL
15 mM 0.1306 mL 0.6528 mL 1.3055 mL 3.2638 mL
20 mM 0.0979 mL 0.4896 mL 0.9791 mL 2.4479 mL
25 mM 0.0783 mL 0.3917 mL 0.7833 mL 1.9583 mL
30 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6319 mL
40 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2239 mL
50 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9791 mL
60 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
80 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
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VRT-325 Related Classifications

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.

Keywords:

VRT-325815592-21-3VRT325VRT 325CFTRCystic fibrosis transmembrane conductance regulatorHEK 293 cellsendoplasmic reticulumP-gpnucleotide-binding domain 1P-glycoproteincystic fibrosisCFBE-ΔF508 cellsprimary human cystic fibrosis airway epithelial cellsΔF508-CFTRInhibitorinhibitorinhibit

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