Pimavanserin tartrate

SKU: orb1300322

Description

Pimavanserin tartrate is a selective 5-HT2A receptor inverse agonist employed in research on Parkinson's disease psychosis. It potently inhibits the NFAT signaling pathway and is utilized in both in vitro receptor studies and in vivo models of neuropsychiatric disorders.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	706782-28-7
MW	1005.2
Purity	>99.99% (May vary between batches)
Formula	C₅₀H₆₈F₂N₆O₄·C₄H₆O₆
SMILES	O[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
Target	5-HT Receptor
Solubility	Ethanol:93 mg/mL (92.52 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (2.49 mM);DMSO:28.05 mg/mL (27.9 mM);H2O:92 mg/mL (91.52 mM)

Bioactivity

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Target IC50	5-HT2A:8.7(pIC50)
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. 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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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ACP103, ACP-103, ACP-103 hemitartrate, ACP103 Tartrate, ACP 103, ACP 103 Tartrate, 5-HT Receptor, 5-HT2A, 5HT Receptor, 5HTReceptor, Pimavanserin hemitartrate

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Compound Identifiers

PubChem CID

11672491 ↗

Key Properties

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No computed properties available.

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