| 名称 | Pimavanserin tartrate |
| 描述 | Pimavanserin tartrate is a potent 5-HT 2A receptor inverse agonist used to treat Parkinson's disease-related psychosis, with the most potent inhibitory activity on the NFAT signaling pathway. |
| 体外活性 | METHODS: The pharmacological effects of PVT on TNBC cells were evaluated at specific time points and different concentration ranges (1.25-20 μM). The short-term effects (24-72 hours) of PVT treatment on the proliferation of two TNBC cell lines, 4T1 and MDA-MB-231, were evaluated using MTT assay.
RESULTS The half-maximal inhibitory concentration (IC50) values of PVT on 4T1 cell line at 24 hours, 48 hours and 72 hours were 6.77 μM, 1.94 μM and 1.46 μM, respectively, while the half-maximal inhibitory concentration (IC50) values for MDA-MB-231 were 9.65 μM, 4.24 μM and 2.31 μM, respectively. The inhibitory effect of PVT on the viability of 4T1 and MDA-MB-231 cells showed concentration dependence. However, PVT has a smaller inhibitory effect on the viability of normal human breast epithelial MCF-10A cells.[1] |
| 体内活性 | METHODS: Mice were inoculated with 1 × 105 luciferase-expressing 4T1 cells into the left peritoneal cavity. PVT (30 mg/kg) was administered daily by intraperitoneal injection. When the average tumor volume reached approximately 1000 mm3, the tumors were carefully excised and the wounds sutured. To monitor metastasis, a non-invasive in vivo imaging system was used to detect tumor metastasis. The data were collected and analyzed using Living Image® 4.7.2 software.
RESULTS PVT mildly inhibited the growth of subcutaneous tumors in vivo without causing significant weight loss in the animals. [1]
METHODS: U87 cells were subcutaneously implanted into nude mice to establish a GBM xenograft model. The mice were treated with Pimavanserin tartrate (10 mg/kg, orally, daily, for three weeks), and the tumor growth in the mice was observed.
RESULTS Pimavanserin tartrate significantly inhibited tumor growth. [2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 93 mg/mL (92.5 mM)
DMSO : 60 mg/mL (59.69 mM)
H2O : 92 mg/mL (91.5 mM)
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| 关键字 | Inhibitor | Pimavanserin hemitartrate | 5-hydroxytryptamine Receptor | ACP-103 Tartrate | ACP-103 hemitartrate | ACP 103 Tartrate | inhibit | Pimavanserin tartrate | 5-HT Receptor | ACP103 Tartrate | ACP 103 | Serotonin Receptor | ACP103 | Pimavanserin Tartrate |
| 相关产品 | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| 相关库 | 经典已知活性库 | 疼痛相关化合物库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 抗癌上市药物库 | FDA 上市药物库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
