产品
编 号：F104024
分子式：C20H24ClN3O2
分子量：373.88
分子式：C20H24ClN3O2
分子量：373.88
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1265917-14-3
产品详情
生物活性：
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.
体内研究：
S1RA hydrochloride (腹腔注射 16-80 mg/kg 或口服 32-128 mg/kg；一次) 剂量依赖性地抑制小鼠中福尔马林诱导的痛觉，辣椒素诱导的机械超敏反应和坐骨神经损伤诱导的机械和热超敏反应。Animal Model:Male CD1 mice
Dosage:32, 64, 128 and 160 mg/kg
Administration:Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
Result:Reduced the permanence time on the rotating rod in rotarod test.
Animal Model:Male CD1 mice with formalin-evoked nociception
Dosage:20, 40 and 80 mg/kg
Administration:Intraperitoneal injection; 20, 40 and 80 mg/kg, once
Result:Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
Animal Model:Male CD1 mice with capsaicin-induced mechanical hypersensitivity
Dosage:16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
Administration:Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
Result:Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
体外研究：
S1RA hydrochloride (0.1-10000 nM) 对人和豚鼠的 σ1R 的 Ki 值分别为 17 和 23.5nM。 S1RA hydrochloride (0.1-10000 nM) 对人 σ2R 具有亲和力，Ki 值为 9.3 μM。 S1RA hydrochloride 对人 5-HT2B 受体具有亲和力，Ki 值为 328 nM，IC50 值为 4.7 μM。
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.
体内研究：
S1RA hydrochloride (腹腔注射 16-80 mg/kg 或口服 32-128 mg/kg；一次) 剂量依赖性地抑制小鼠中福尔马林诱导的痛觉，辣椒素诱导的机械超敏反应和坐骨神经损伤诱导的机械和热超敏反应。Animal Model:Male CD1 mice
Dosage:32, 64, 128 and 160 mg/kg
Administration:Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
Result:Reduced the permanence time on the rotating rod in rotarod test.
Animal Model:Male CD1 mice with formalin-evoked nociception
Dosage:20, 40 and 80 mg/kg
Administration:Intraperitoneal injection; 20, 40 and 80 mg/kg, once
Result:Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
Animal Model:Male CD1 mice with capsaicin-induced mechanical hypersensitivity
Dosage:16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
Administration:Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
Result:Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
体外研究：
S1RA hydrochloride (0.1-10000 nM) 对人和豚鼠的 σ1R 的 Ki 值分别为 17 和 23.5nM。 S1RA hydrochloride (0.1-10000 nM) 对人 σ2R 具有亲和力，Ki 值为 9.3 μM。 S1RA hydrochloride 对人 5-HT2B 受体具有亲和力，Ki 值为 328 nM，IC50 值为 4.7 μM。
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