Description In vitro In vivo
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iOWH-032

Description In vitro In vivo
Product Name
iOWH-032
CAS No.
1191252-49-9
Chemical Name
iOWH-032
Synonyms
CS-950;iOWH-032;IOWH032;IOWH 032;iOWH-032 USP/EP/BP;IOWH-032; IOWH032; IOWH 032;3-(3,5-DibroMo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxaMide;3-(3,5-Dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-1,2,4-oxadiazole-5-carboxamide;1,2,4-Oxadiazole-5-carboxamide, 3-(3,5-dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-;3-(3,5-DIBROMO-4-OXOCYCLOHEXA-2,5-DIEN-1-YLIDENE)-N-[(4-PHENOXYPHENYL)METHYL]-1,2,4-OXADIAZOLE-5-CARBOXAMIDE;3-(3,5-Dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-1,2,4-oxadiazole-5-carboxamide IOWH032
CBNumber
CB42666789
Molecular Formula
C22H15Br2N3O4
Formula Weight
545.18
MOL File
1191252-49-9.mol
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iOWH-032 Property

Density 
1.670±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
≥21.85 mg/mL in DMSO; insoluble in H2O; ≥3.13 mg/mL in EtOH with gentle warming
form 
solid
pka
3.34±0.46(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

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

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

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N-Bromosuccinimide Price

TRC
Product number
I737013
Product name
IOWH032
Packaging
50mg
Price
$360
Updated
2021/12/16
AK Scientific
Product number
2156AH
Product name
3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide
Packaging
25mg
Price
$231
Updated
2021/12/16
ChemScene
Product number
CS-1744
Product name
IOWH-032
Purity
99.66%
Packaging
100mg
Price
$250
Updated
2021/12/16
AK Scientific
Product number
2156AH
Product name
3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide
Packaging
50mg
Price
$305
Updated
2021/12/16
AK Scientific
Product number
2156AH
Product name
3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide
Packaging
10mg
Price
$150
Updated
2021/12/16
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iOWH-032 Chemical Properties,Usage,Production

Description

IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. Phase 2.

In vitro

IOWH032 shows inhibitory activity against CFTR in T84-CFTR cell based assays with IC50 of 6.87 μM.

In vivo

In a mouse closed-loop model, IOWH032 causes a statistical significant inhibition against cholera toxin (CTX) induced secretion. IOWH032 (5 mg/kg) reduces the fecal output index by ~70% in a cecetomized rat model.

Uses

IOWH032 is a synthetic?cystic fibrosis transmembrane conductance regulator (CFTR) ?inhibitor.

Biological Activity

iowh-032 is a potent and synthetic extracellular cystic fibrosis transmembrane conductance regulator (cftr) inhibitor with ic50 value of 1.01 μm in t84 and cho-cftr cell based assays [1]. the cftr chloride channel is the most attractive because it is the primary driver of secretion in cases of diarrhea caused by enterotoxigenic bacteria. cftr plays an important role in transepithelial fluid homeostasis through controlling the flow of chloride ions and thus the movement of water in and out of cells [1].

in vitro

iowh032 inhibited cftr activity with ic50 value of 6.87 μm in t84-cftr cell based assays [1]. iowh-032 rapidly blocked and potentiated hcftr activity in a concentration-dependent manner with apparent kd value of 6.1 nm and 0.64 nm, respectively. however, iowh-032 did not potentiate and only blocked mcftr with an apparent kd value of 42.9 μm [2].

in vivo

iowh032 significantly inhibited cholera toxin (ctx)-induced secretion in a mouse closed-loop model. moreover, iowh032 (5 mg/kg, po dose) decreased the fecal output index by apparent 70% compared to vehicle (cholera toxin) in a cecetomized rat model. iowh032 inhibited cftr activity with ic50 value of 6.87 μm in t84-cftr cell based assays [1].

target

cftr

IC 50

1.01 μm

References

1. doyle k, et al. inhibitors of the cftr chloride ion channel as potential treatment for acute secretory diarrhea: development of 5-membered heterocycles suitable for pre-clinical evaluation.1. de hostos el, choy rk, nguyen t. developing novel antisecretory drugs to treat infectious diarrhea. future med chem. 2011;3(10):1317-25. 2. cui g, khazanov n, stauffer b, infield dt, imhoff br, senderowitz h, et al. potentiators exert distinct effects on human, murine, and xenopus cftr. am j physiol lung cell mol physiol. 2016:ajplung 00056 2016.

iOWH-032 Preparation Products And Raw materials

Raw materials

Preparation Products

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iOWH-032 Suppliers

MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
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InvivoChem
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Aladdin Scientific
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Matrix Scientific
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View Lastest Price from iOWH-032 manufacturers

Career Henan Chemical Co
Product
iOWH-032 1191252-49-9
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2020-01-13

1191252-49-9, iOWH-032Related Search:


  • 3-(3,5-DibroMo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxaMide
  • 3-(3,5-DIBROMO-4-OXOCYCLOHEXA-2,5-DIEN-1-YLIDENE)-N-[(4-PHENOXYPHENYL)METHYL]-1,2,4-OXADIAZOLE-5-CARBOXAMIDE
  • iOWH-032
  • 3-(3,5-Dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-1,2,4-oxadiazole-5-carboxamide
  • IOWH-032; IOWH032; IOWH 032
  • CS-950
  • IOWH032;IOWH 032
  • 1,2,4-Oxadiazole-5-carboxamide, 3-(3,5-dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-
  • 3-(3,5-Dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-1,2,4-oxadiazole-5-carboxamide IOWH032
  • iOWH-032 USP/EP/BP
  • 1191252-49-9
  • C22H15Br2N3O4
  • Inhibitors