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编 号：F015593
分子式：C24H29N3O8
分子量：487.5
分子式：C24H29N3O8
分子量：487.5
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CAS No: 1035654-66-0
产品详情
生物活性：
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne.
体内研究：
Sarecycline hydrochloride (0.33-9 mg /kg; 静脉注射) 在小鼠中性粒细胞减少的大腿感染模型中显示出对金黄色葡萄球菌的有效活性。Sarecycline 在全身 (腹腔) 感染的 CD-1 小鼠模型中能够抑制金黄色葡萄糖球菌 (PD50=0.25 mg/kg)，但在最高剂量 (>40 mg/kg) 下对大肠杆菌抑制的效果不明显。Sarecycline (1-150mg/kg; 腹腔注射; 单剂量) 在 Sprague Dawley 大鼠模型中具有抗炎活性。Animal Model:Carrageenan-induced footpad edema male Sprague Dawley rats model
Dosage:1 mg/kg, 5 mg/kg ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg,100 mg/kg, 150 mg/kg
Administration:Intraperitoneal injection (i.p.); Single dose. Before a subplantar injection of sterile 1 mg/0.1 mL carrageenan solution in the right hind paw.
Result:Reduced inflammation to 55.7% and 53.1%, respectively, at doses of 75 mg/kg and 100 mg/kg compared to baseline.
Animal Model:Carrageenan-induced footpad edema male Sprague Dawley rats model
Dosage:0.33, 1, 3, or 9?mg/kg
Administration:Intravenously
Result:Achieved a 2-log10 reduction in the bacterial burden in the thigh at a dose comparable to that of doxycycline, with ED50s of 8.23 and 8.32?mg/kg, respectively.
体外研究：
Sarecycline 抑制 55 株临床分离的痤疮棒状杆菌，其 MIC 值为 0.5~16 μg/ml; MIC50 为 0.5 μg/ml, MIC90 为 4μg/ml。Sarecycline 对大环内酯耐药的生物体有活性。Sarecycline hydrochloride对肠道需氧革兰氏阴性菌的活性最小。
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne.
体内研究：
Sarecycline hydrochloride (0.33-9 mg /kg; 静脉注射) 在小鼠中性粒细胞减少的大腿感染模型中显示出对金黄色葡萄球菌的有效活性。Sarecycline 在全身 (腹腔) 感染的 CD-1 小鼠模型中能够抑制金黄色葡萄糖球菌 (PD50=0.25 mg/kg)，但在最高剂量 (>40 mg/kg) 下对大肠杆菌抑制的效果不明显。Sarecycline (1-150mg/kg; 腹腔注射; 单剂量) 在 Sprague Dawley 大鼠模型中具有抗炎活性。Animal Model:Carrageenan-induced footpad edema male Sprague Dawley rats model
Dosage:1 mg/kg, 5 mg/kg ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg,100 mg/kg, 150 mg/kg
Administration:Intraperitoneal injection (i.p.); Single dose. Before a subplantar injection of sterile 1 mg/0.1 mL carrageenan solution in the right hind paw.
Result:Reduced inflammation to 55.7% and 53.1%, respectively, at doses of 75 mg/kg and 100 mg/kg compared to baseline.
Animal Model:Carrageenan-induced footpad edema male Sprague Dawley rats model
Dosage:0.33, 1, 3, or 9?mg/kg
Administration:Intravenously
Result:Achieved a 2-log10 reduction in the bacterial burden in the thigh at a dose comparable to that of doxycycline, with ED50s of 8.23 and 8.32?mg/kg, respectively.
体外研究：
Sarecycline 抑制 55 株临床分离的痤疮棒状杆菌，其 MIC 值为 0.5~16 μg/ml; MIC50 为 0.5 μg/ml, MIC90 为 4μg/ml。Sarecycline 对大环内酯耐药的生物体有活性。Sarecycline hydrochloride对肠道需氧革兰氏阴性菌的活性最小。
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