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Nesolicaftor (PTI-428) CFTR activator

Name: Nesolicaftor (PTI-428)
Brand: Selleck Chemicals
SKU: S6911
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6911

Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier that increases CFTR expression.

Chemical Structure

Molecular Weight: 354.36

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Quality Control

Batch: S691101 DMSO]71 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.83%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.83

Related Targets	CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other CFTR Inhibitors	Tezacaftor (VX-661) VX-445 (Elexacaftor) Vanzacaftor (VX-121) VX-561(CTP-656) CFTRinh-172 GLPG1837 GlyH-101 FDL169 Galicaftor (ABBV-2222) IOWH032

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (200.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	354.36	Formula	C₁₈H₁₈N₄O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1953130-87-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	CFTR
References	[1] https://pubmed.ncbi.nlm.nih.gov/29055231/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03500263	Completed	Cystic Fibrosis	Proteostasis Therapeutics Inc.	January 30 2018	Phase 1\|Phase 2
NCT03251092	Completed	Healthy Volunteer - Complete\|Cystic Fibrosis - Complete	Proteostasis Therapeutics Inc.	July 17 2017	Phase 1\|Phase 2

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Handling Instructions

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