产品
编 号：F743395
分子式：C27H34ClFN2O4
分子量：505.02
分子式：C27H34ClFN2O4
分子量：505.02
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1233926-87-8
产品详情
生物活性：
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.
体内研究：
PKRA83 (20 mg/kg；腹腔注射) 在胶质母细胞瘤异种移植肿瘤模型中显示出抗肿瘤活性。PKRA83 (15 mg/kg；腹膜内注射，每天一次，持续 2 周) 可抑制患有胶原诱导性关节炎的小鼠的关节炎。Animal Model:glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model
Dosage:20 mg/kg
Administration:i.p, daily
Result:Decreased tumor growth rate and tumor weight.Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
Animal Model:Collagen-induced arthritis in mice
Dosage:15 mg/kg
Administration:i.p, daily for 2 weeks
Result:Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).Lowered IL-1β and 1 L-6 gene expression levels in the joints.
体外研究：
PKRA83 (1 μg/mL) 可有效减少 PK2 诱导的体外微血管内皮细胞分支。PKRA83 (2 μM，24 小时) 阻断 rPK2 在多巴胺能 N27 细胞中的神经保护作用 (rPK2 保护 N27 细胞免受 MPP+ 诱导的多巴胺能神经元细胞死亡)。
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.
体内研究：
PKRA83 (20 mg/kg；腹腔注射) 在胶质母细胞瘤异种移植肿瘤模型中显示出抗肿瘤活性。PKRA83 (15 mg/kg；腹膜内注射，每天一次，持续 2 周) 可抑制患有胶原诱导性关节炎的小鼠的关节炎。Animal Model:glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model
Dosage:20 mg/kg
Administration:i.p, daily
Result:Decreased tumor growth rate and tumor weight.Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
Animal Model:Collagen-induced arthritis in mice
Dosage:15 mg/kg
Administration:i.p, daily for 2 weeks
Result:Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).Lowered IL-1β and 1 L-6 gene expression levels in the joints.
体外研究：
PKRA83 (1 μg/mL) 可有效减少 PK2 诱导的体外微血管内皮细胞分支。PKRA83 (2 μM，24 小时) 阻断 rPK2 在多巴胺能 N27 细胞中的神经保护作用 (rPK2 保护 N27 细胞免受 MPP+ 诱导的多巴胺能神经元细胞死亡)。
产品资料
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