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Pimavanserin tartrate 5-HT Receptor inhibitor

Name: Pimavanserin tartrate
Brand: Selleck Chemicals
SKU: S8183
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S8183

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.

Chemical Structure

Molecular Weight: 1005.2

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR Histamine Receptor Dopamine Receptor Ras KRas GPR
Other 5-HT Receptor Inhibitors	WAY-100635 Maleate Puerarin Serotonin (5-HT) HCl SB269970 HCl Ketanserin BRL-15572 Dihydrochloride Nuciferine RS-127445 Flopropione Azacyclonol

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (99.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 25 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (4.97mM)	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 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (1.24mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	1005.2	Formula	C₅₀H₆₈F₂N₆O₄.C₄H₆O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	706782-28-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ACP-103			Smiles	CC(C)COC1=CC=C(C=C1)CNC(=O)N(CC2=CC=C(C=C2)F)C3CCN(CC3)C.CC(C)COC1=CC=C(C=C1)CNC(=O)N(CC2=CC=C(C=C2)F)C3CCN(CC3)C.C(C(C(=O)O)O)(C(=O)O)O

Mechanism of Action

Targets/IC₅₀/Ki	5-HT2A (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. In a rat model of parkinsonian tremor, Pimavanserin (40 mg/kg, i.p.) produces a significant overall reduction of tacrine-induced tremulous jaw movements.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16469866/ [2] https://pubmed.ncbi.nlm.nih.gov/18534670/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05796167	Recruiting	Parkinson Disease	State University of New York - Downstate Medical Center\|ACADIA Pharmaceuticals Inc.	April 4 2024	Early Phase 1
NCT05555615	Recruiting	Irritability Associated With Autism Spectrum Disorder	ACADIA Pharmaceuticals Inc.	November 2 2022	Phase 2\|Phase 3
NCT04794413	Completed	Tourette Syndrome\|Tardive Dyskinesia	Joseph Jankovic\|Andrew Billnitzer MD\|Baylor College of Medicine	November 12 2018	Early Phase 1
NCT03121586	Active not recruiting	Schizophrenia	ACADIA Pharmaceuticals Inc.	January 2017	Phase 3
NCT00087542	Completed	Hallucinations\|Psychoses\|Parkinson''s Disease	ACADIA Pharmaceuticals Inc.	March 2004	Phase 2

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