iOWH-032

Bezeichnung:iOWH-032

CAS-Nr1191252-49-9

Englisch Name:iOWH-032

CBNumberCB42666789

SummenformelC22H15Br2N3O4

Molgewicht545.18

MOL-Datei1191252-49-9.mol

iOWH-032 physikalisch-chemischer Eigenschaften

Dichte	1.670±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	≥21.85 mg/mL in DMSO; insoluble in H2O; ≥3.13 mg/mL in EtOH with gentle warming
Aggregatzustand	solid
pka	3.34±0.46(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

iOWH-032 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
IOWH032 is a synthetic?cystic fibrosis transmembrane conductance regulator (CFTR) ?inhibitor.
Biologische Aktivität
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
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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