ChemicalBook > CAS DataBase List > CFTRinh-172

CFTRinh-172

Product Name
CFTRinh-172
CAS No.
307510-92-5
Chemical Name
CFTRinh-172
Synonyms
CS-1067;CFTR(INH)-172;CFTR INHIBITOR-172;CFTRinh-172 USP/EP/BP;InSolution? CFTR Inhibitor-172;CFTR INHIBITOR-172;CFTRINH-172;CFTRinh 172 (CFTR Inhibitor-172);CFTR Inhibitor-172 - CAS 307510-92-5 - Calbiochem;InSolution CFTR Inhibitor-172 - CAS 307510-92-5 - Calbiochem;4-[[4-Oxo-2-Thioxo-3-[3-(Trifluoromethyl)Phenyl]Thiazolidin-
CBNumber
CB0364629
Molecular Formula
C18H10F3NO3S2
Formula Weight
409.4
MOL File
307510-92-5.mol
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CFTRinh-172 Property

Melting point:
181-183 °C
Boiling point:
555.7±60.0 °C(Predicted)
Density 
1.61±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: ≥10mg/mL
form 
Yellow solid
pka
3.88±0.10(Predicted)
color 
yellow
CAS DataBase Reference
307510-92-5
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Safety

Hazard Codes 
Xi,N
Risk Statements 
36/37/38-43-50/53
Safety Statements 
26-36/37-60-61
RIDADR 
UN 3077 9 / PGIII
WGK Germany 
3
HazardClass 
IRRITANT
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H317May cause an allergic skin reaction

H319Causes serious eye irritation

H335May cause respiratory irritation

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
219670
Product name
CFTR Inhibitor-172
Packaging
5mg
Price
$187
Updated
2024/03/01
Sigma-Aldrich
Product number
219674
Product name
InSolution? CFTR Inhibitor-172
Packaging
5mg
Price
$195
Updated
2023/01/07
Cayman Chemical
Product number
15545
Product name
CFTR Inhibitor-172
Purity
≥98%
Packaging
5mg
Price
$81
Updated
2024/03/01
Cayman Chemical
Product number
15545
Product name
CFTR Inhibitor-172
Purity
≥98%
Packaging
10mg
Price
$152
Updated
2024/03/01
Sigma-Aldrich
Product number
C2992
Product name
CFTR(inh)-172
Purity
≥98% (HPLC), powder
Packaging
5mg
Price
$191
Updated
2024/03/01
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CFTRinh-172 Chemical Properties,Usage,Production

Uses

The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR). CFTR Inhibitor-172 is a thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner. It appears to directly modulate the gating of chloride at the channel and does not prevent elevation of cAMP or inhibit other pumps or channels. In mice, CFTR inhibitor-172 prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection. It slows cyst growth in animal models of polycystic kidney disease. As CFTR also modulates glutathione (GSH) efflux, CFTR inhibitor-172 can affect intracellular GSH concentration and reactive oxygen species balance.

Uses

CFTR(inh)-172 has been used to specifically inhibit cystic fibrosis transmembrane conductance regulator (CFTR) activity. It is also used as a CFTR inhibitor Inh-172 to treat forskolin and IBMX.

Definition

ChEBI: A thiazolidinone that is 2-thioxo-4-thiazolidinone which is substituted at position 3 by a (m--trifluoromethyl)phenyl group and at position 5 by a p-carboxybenzylidene group. It is an inhibitor of cystic fibrosis transmembrane con uctance regulator, a membrane protein and chloride channel in vertebrates that is encoded by the CFTR gene.

Biological Activity

Voltage-independent, selective CFTR chloride channel blocker (K i = 300 nM) that alters channel gating. Blocks intestinal fluid secretion induced by cholera toxin and Escherichia coli and suppresses cyst growth in animal models of polycystic kidney disease. Orally active. Inhibits mitochondrial respiration and increases reactive oxygen species (ROS) production independently of CFTR in several cell lines.

Biochem/physiol Actions

CFTR(inh)-172 is an inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR). With a Ki = 300 nM,. CFTR(inh)-172 leads to rapid, reversible and voltage-independent inhibition; it is an antidiarrheal agent in animals. CTFR(inh)-172 may be a useful tool to study animal models of cystic fibrosis and intestinal fluid loss in cholera and other secretory diarrheas. CTFR(inh)-172 is structurally-unrelated to known, but non-specific CFTR inhibitors DPC, NPPB (Cat. No. N4779) and Glibenclamide.

in vitro

cftrinh-172 could reversibly inhibit cftr short-circuit current in less than 2 minutes in a voltage-independent manner. moreover, at concentrations fully inhibiting cftr, cftrinh-172 did not prevent elevation of cellular camp or inhibit non-cftr cl–channels, multidrug resistance protein-1, atp-sensitive k+ channels, or a series of other transporters [2].

in vivo

a single ip injection of cftrinh-172 (250 μg/kg) in mice reduced by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. cftrinh-172 may be useful in developing large-animal models of cystic fibrosis and reducing intestinal fluid loss in cholera and other secretory diarrheas [3].

storage

Store at +4°C

References

[1] ma t, thiagarajah jr, yang h, sonawane nd, folli c, galietta lj, verkman as. thiazolidinone cftr inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. j clin invest. 2002 dec;110(11):1651-8.

CFTRinh-172 Preparation Products And Raw materials

Raw materials

Preparation Products

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CFTRinh-172 Suppliers

MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
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United States
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View Lastest Price from CFTRinh-172 manufacturers

Career Henan Chemical Co
Product
CFTRinh-172 307510-92-5
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
20kg
Release date
2019-12-23

307510-92-5, CFTRinh-172Related Search:


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