[CAS NO. 307510-92-5] CFTR(inh)-172
PRODUCTS SPECIFICATIONS [307510-92-5]
DESCRIPTION [307510-92-5]
Overview
| MDL | MFCD01164609 |
|---|---|
| Molecular Weight | 409.40 |
| Molecular Formula | C18H10F3NO3S2 |
| 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 |
4 Publications Citing Use of MCE
Summary
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 K i of 300 nM.
IC50 & Target
Ki: 300 nM (CFTR) [1]
In Vitro
Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t 1/2 =4 minutes) and is reversed after ishout with t 1/2 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 K i =0.6 μM. This effect is due to increased mean channel closed time without changing mean channel open time. The K i values for inhibition of Cl - current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, K i 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.
Appearance
Solid
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
DMSO : 50 mg/mL ( 122.13 mM ; Need ultrasonic)
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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution
References
- [1] Ma T, et al. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.
- [2] Taddei A, et al. Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett. 2004 Jan 30;558(1-3):52-6.
Synonyms