产品
编 号：F742796
分子式：C17H16N6O3S
分子量：384.41
分子式：C17H16N6O3S
分子量：384.41
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CAS No: 1160498-08-7
产品详情
生物活性：
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
体内研究：
COX-2-IN-30 (化合物 7a) (10 mg/kg；口服；单剂量) 表现出镇痛活性，同时显着减少小鼠的扭动次数。COX-2-IN-30 (10 mg/kg；口服；单次剂量) 在 Carrageenan (HY-125474) 诱导的大鼠爪水肿试验中导致爪高度显着降低。 COX-2-IN-30 显着降低 TNF-α 和 IL-1β 的水平。COX-2-IN-30 (10 mg/kg；口服；单剂量) 在雄性白化病大鼠的胃组织中表现出安全性。Animal Model:Albino mice (25-30 g)
Dosage:10 mg/kg
Administration:PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
Result:Decreased the number of writhing responses of mouse conpared with control group.
Animal Model:Paw edema rat induced by Carrageenan (HY-125474)
Dosage:10 mg/kg
Administration:PO; single dose; after one hour, 0.1?mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3?h
Result:Showed a significant reduction of paw height compared to control after 3 h.
体外研究：
COX-2-IN-30 (化合物 7a) 与 hCA 亚型结合，Ki 值分别为 183.4 nM (hCA I)、81.4 nM (hCA II)、38.4 nM (hCA IX)、21.6 nM (hCA XII)。
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
体内研究：
COX-2-IN-30 (化合物 7a) (10 mg/kg；口服；单剂量) 表现出镇痛活性，同时显着减少小鼠的扭动次数。COX-2-IN-30 (10 mg/kg；口服；单次剂量) 在 Carrageenan (HY-125474) 诱导的大鼠爪水肿试验中导致爪高度显着降低。 COX-2-IN-30 显着降低 TNF-α 和 IL-1β 的水平。COX-2-IN-30 (10 mg/kg；口服；单剂量) 在雄性白化病大鼠的胃组织中表现出安全性。Animal Model:Albino mice (25-30 g)
Dosage:10 mg/kg
Administration:PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
Result:Decreased the number of writhing responses of mouse conpared with control group.
Animal Model:Paw edema rat induced by Carrageenan (HY-125474)
Dosage:10 mg/kg
Administration:PO; single dose; after one hour, 0.1?mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3?h
Result:Showed a significant reduction of paw height compared to control after 3 h.
体外研究：
COX-2-IN-30 (化合物 7a) 与 hCA 亚型结合，Ki 值分别为 183.4 nM (hCA I)、81.4 nM (hCA II)、38.4 nM (hCA IX)、21.6 nM (hCA XII)。
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