1. Membrane Transporter/Ion Channel
    Autophagy
  2. CFTR
    Autophagy
  3. CFTR(inh)-172

CFTR(inh)-172 

Cat. No.: HY-16671 Purity: 98.70%
Handling Instructions

CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.

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

CFTR(inh)-172 Chemical Structure

CFTR(inh)-172 Chemical Structure

CAS No. : 307510-92-5

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Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 85 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 77 In-stock
Estimated Time of Arrival: December 31
10 mg USD 128 In-stock
Estimated Time of Arrival: December 31
50 mg USD 495 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.

IC50 & Target

Ki: 300 nM (CFTR)[1]

In Vitro

Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t1/2=4 minutes) and is reversed after ishout with t1/2 approximately 5 minutes. CFTRinh-172 is nontoxic to FRT cells after 24 hours at concentrations up to 100 μM[1]. CFTR(inh)-172 does not alter CFTR unitary conductance (8 pS), but reduces open probability by > 90% with Ki=0.6 μM. This effect is due to increased mean channel closed time without changing mean channel open time. The Ki values for inhibition of Cl- current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, Ki is significantly reduced to 0.2 μM for vF508 CFTR[2].

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

In Vivo

A single intraperitoneal injection of CFTR(inh)-172 (250 μg/kg) in mice reduces by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTR(inh)-172 is nontoxic at high concentrations in mouse models. CFTRinh-172 significantly reduces fluid secretion to that in saline control loops, whereas an inactive CFTRinh-172 analog does not inhibit fluid secretion[1].

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

Molecular Weight

409.40

Formula

C18H10F3NO3S2

CAS No.
SMILES

S=C(S/1)N(C2=CC=CC(C(F)(F)F)=C2)C(C1=C\C3=CC=C(C=C3)C(O)=O)=O

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 : 50 mg/mL (122.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4426 mL 12.2130 mL 24.4260 mL
5 mM 0.4885 mL 2.4426 mL 4.8852 mL
10 mM 0.2443 mL 1.2213 mL 2.4426 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.11 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

*All of the co-solvents are available by MCE.
References
Cell Assay
[1]

CFTR(inh)-172 is diluted in DMSO as a 10 mM stock solution and diluted with appropriate medium. Fischer rat thyroid (FRT) cells coexpressing human wild-type CFTR and the halide indicator YFP-H148Q are generated. Cell toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor CFTR(inh)-172[1].

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

Animal Administration
[1]

Mice: Animal toxicity is assessed by measurement of serum chemistries and hematology in mice at 5 days after daily intraperitoneal injections with 0-1,000 μg/kg CFTR(inh)-172[1].

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

References
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Product Name:
CFTR(inh)-172
Cat. No.:
HY-16671
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