Pimavanserin tartrate

Catalog No.S8183 Batch:S818303

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Technical Data

Formula

C50H68F2N6O4.C4H6O6
Molecular Weight 1005.2 CAS No. 706782-28-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (99.48 mM)
Water 100 mg/mL (99.48 mM)
Ethanol 25 mg/mL (24.87 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Pimavanserin tartrate(ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.
Targets
5-HT2A [1]
(cell-based assay)
8.7(pIC50)
In vivo

In rats, Pimavanserin (3 mg/kg, p.o.) attenuates DOI-induced head twitches. In mice, Pimavanserin (3 mg/kg, p.o.) significantly attenuates MK-801-induced hyperactivity. [1] In a rat model of parkinsonian tremor, Pimavanserin (40 mg/kg, i.p.) produces a significant overall reduction of tacrine-induced tremulous jaw movements. [2]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    3 mg/kg

  • Administration

    p.o.

Selleck's Pimavanserin tartrate has been cited by 3 publications

A new class of serotonin 5-HT2A /5-HT2C receptor inverse agonists: Synthesis, molecular modeling, in vitro and in vivo pharmacology of novel 2-aminotetralins [ Br J Pharmacol, 2021, 10.1111/bph.15756] PubMed: 34837227
Repurposing Pimavanserin, an Anti-Parkinson Drug for Pancreatic Cancer Therapy [ Mol Ther Oncolytics, 2020, 19:19-32] PubMed: 33024816
Discovery of Procognitive Antipsychotics by Combining Muscarinic M1 Receptor Structure-Activity Relationship with Systems Response Profiles in Zebrafish Larvae [ ACS Chem Neurosci, 2020, 11(2):173-183] PubMed: 31850734

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.