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Pimavanserin tartrate

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Catalog No. T6946Cas No. 706782-28-7
Alias ACP-103

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.

Pimavanserin tartrate

Pimavanserin tartrate

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Purity: 99.98%
Catalog No. T6946Alias ACP-103Cas No. 706782-28-7
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$43In StockIn Stock
50 mg$68In StockIn Stock
100 mg$108In StockIn Stock
200 mg$146In StockIn Stock
500 mg$242In StockIn Stock
1 mL x 10 mM (in DMSO)$29In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.98%
Color:White
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Product Introduction

Bioactivity
Description
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.
Targets&IC50
5-HT2A:8.7(pIC50)
In vitro
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]
In vivo
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]
SynonymsACP-103
Chemical Properties
Molecular Weight1005.2
FormulaC50H68F2N6O4·C4H6O6
Cas No.706782-28-7
SmilesO[C@H]([C@@H](O)C(O)=O)C(O)=O.CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C)CC2)cc1.CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C)CC2)cc1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 93 mg/mL (92.52 mM), Sonication is recommended.
DMSO: 28.05 mg/mL (27.9 mM), Sonication is recommended.
H2O: 92 mg/mL (91.52 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (2.49 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO/H2O/Ethanol
1mg5mg10mg50mg
1 mM0.9948 mL4.9741 mL9.9483 mL49.7413 mL
5 mM0.1990 mL0.9948 mL1.9897 mL9.9483 mL
10 mM0.0995 mL0.4974 mL0.9948 mL4.9741 mL
20 mM0.0497 mL0.2487 mL0.4974 mL2.4871 mL
H2O/Ethanol
1mg5mg10mg50mg
50 mM0.0199 mL0.0995 mL0.1990 mL0.9948 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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