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编 号：F748204
分子式：C24H19F8N5O3S
分子量：609.49
分子式：C24H19F8N5O3S
分子量：609.49
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CAS No: 1984824-54-5
产品详情
生物活性：
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.
体内研究：
GDC-0334 (0-150 mg/kg；静脉注射) 能够减轻大鼠水肿、真皮血流量 (DBF)、咳嗽和过敏性气道炎症。GDC-0334 (静脉注射 0.5/1 mg/kg，口服 1/5 mg/kg) 显示静脉注射 T1/2 为 11.9 小时 (小鼠) 和 9.79 小时 (大鼠) ，口服生物利用度 (F%) 为 45.0% (小鼠) 和 46.2% (大鼠)。 Pharmacokinetic parameters for GDC-0334 in mouse/rat/dog/monkey SpeciesIV DoseCL (ml/min/kg)VSS (liter/kg)T1/2 (h) PO Dose(mg/kg)Oral F(%)
Mouse0.512.413.911.9145.0
Rat17.685.559.79546.2
Dog17.576.9728.0527.1
Monkey114.95.417.75513.4
Animal Model:Mouse, rat, dog, monkey (Pharmacokinetic assay)
Dosage:0.5,1,5 mg/kg
Administration:Intravenous injection (i.v.), oral gavage (p.o.)
Result:Showed a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats .
Animal Model:Rats/guinea pigs model of cough
Dosage:3,10,35,70,75,150 mg/kg
Administration:Intravenous injection (i.v.)
Result:Suppressed AITC-induced edema in vivo in rat. Caused a dose-dependent reduction in AITC-induced dermal blood flow in guinea pigs. Reduced airway airway allergic inflammation in rats and guinea pigs as well as cough in guinea pigs.
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.
体内研究：
GDC-0334 (0-150 mg/kg；静脉注射) 能够减轻大鼠水肿、真皮血流量 (DBF)、咳嗽和过敏性气道炎症。GDC-0334 (静脉注射 0.5/1 mg/kg，口服 1/5 mg/kg) 显示静脉注射 T1/2 为 11.9 小时 (小鼠) 和 9.79 小时 (大鼠) ，口服生物利用度 (F%) 为 45.0% (小鼠) 和 46.2% (大鼠)。 Pharmacokinetic parameters for GDC-0334 in mouse/rat/dog/monkey SpeciesIV DoseCL (ml/min/kg)VSS (liter/kg)T1/2 (h) PO Dose(mg/kg)Oral F(%)
Mouse0.512.413.911.9145.0
Rat17.685.559.79546.2
Dog17.576.9728.0527.1
Monkey114.95.417.75513.4
Animal Model:Mouse, rat, dog, monkey (Pharmacokinetic assay)
Dosage:0.5,1,5 mg/kg
Administration:Intravenous injection (i.v.), oral gavage (p.o.)
Result:Showed a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats .
Animal Model:Rats/guinea pigs model of cough
Dosage:3,10,35,70,75,150 mg/kg
Administration:Intravenous injection (i.v.)
Result:Suppressed AITC-induced edema in vivo in rat. Caused a dose-dependent reduction in AITC-induced dermal blood flow in guinea pigs. Reduced airway airway allergic inflammation in rats and guinea pigs as well as cough in guinea pigs.
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