| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Pimavanserin tartrate (formerly known as BVF036; ACP-103; BVF-036; Nuplazid), the tartrate salt of Pimavanserin, is a novel and orally bioactive inverse agonist of the 5-HT2A (serotonin receptor subtype 2A) receptor the has been approved in 2016 as an atypical antipsychotic for the treatment of Parkinson's disease psychosis.
| Targets |
5-HT2A ( pIC50 = 8.7 )
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|---|---|
| ln Vitro |
Pimavanserin hemitartrate competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT 2A receptors with an average pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin hemitartrate demonstrated potent inverse agonist activity in a cell-based functional assay Receptor Selection and Ascending Technology (R-SAT) with an average pIC50 of 8.7. Pimavanserin hemitartrate exhibits low affinity (average pKi 8.80 in membranes and 8.00 in whole cells, determined by binding to ligand) and potency as an inverse agonist (average pIC50 7.1 in R-SAT) against human 5 -HT 2C absorption, lacks affinity and functional activity for 5-HT 2B absorption, dopamine D2 absorption and other human monoaminergic absorption [1].
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| ln Vivo |
Pimavanserin (3 mg/kg, p.o.) attenuates head twitches caused by DOI in rats. Pimavanserin (3 mg/kg, p.o.) significantly reduces the hyperactivity induced by MK-801 in mice. [1] Pimavanserin (40 mg/kg, i.p.) significantly reduces tacrine-induced tremulous jaw movements in a rat model of parkinsonian tremor. [2]
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| Animal Protocol |
Male Sprague-Dawley rats
3 mg/kg p.o. |
| References |
| Molecular Formula |
C54H74F2N6O10
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|---|---|
| Molecular Weight |
1005.21
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| Exact Mass |
1005.21
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| Elemental Analysis |
C, 64.52; H, 7.42; F, 3.78; N, 8.36; O, 15.92
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| CAS # |
706782-28-7
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| Related CAS # |
Pimavanserin; 706779-91-1
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| Appearance |
Solid powder
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| 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@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
RGSULKHNAKTFIZ-CEAXSRTFSA-N
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| InChi Code |
InChI=1S/2C25H34FN3O2.C4H6O6/c2*1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21;5-1(3(7)8)2(6)4(9)10/h2*4-11,19,23H,12-18H2,1-3H3,(H,27,30);1-2,5-6H,(H,7,8)(H,9,10)/t;;1-,2-/m..1/s1
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| Chemical Name |
(2R,3R)-2,3-dihydroxybutanedioic acid;1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
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| Synonyms |
ACP-103 tartrate; ACP 103; BVF036; ACP-103; BVF-036; ACP103; Trade name: Nuplazid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9948 mL | 4.9741 mL | 9.9482 mL | |
| 5 mM | 0.1990 mL | 0.9948 mL | 1.9896 mL | |
| 10 mM | 0.0995 mL | 0.4974 mL | 0.9948 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03623321 | Active Recruiting |
Drug: Pimavanserin | Neuropsychiatric Symptoms Related to Neurodegenerative Disease |
ACADIA Pharmaceuticals Inc. | July 17, 2018 | Phase 3 |
| NCT04531982 | Active Recruiting |
Drug: Pimavanserin Drug: Placebo |
Schizophrenia | ACADIA Pharmaceuticals Inc. | August 5, 2020 | Phase 3 |
| NCT05441280 | Recruiting | Drug: pimavanserin Other: Placebo |
Post-traumatic Stress Disorder Insomnia |
VA Office of Research and Development |
June 26, 2023 | Phase 2 |
| NCT04373317 | Recruiting | Drug: Pimavanserin Drug: Quetiapine |
Parkinson's Disease Psychosis | VA Office of Research and Development |
October 24, 2022 | Phase 4 |
| NCT06068465 | Recruiting | Drug: pimavanserin tartrate Drug: Placebo |
Parkinson's Disease Psychosis | Tasly Pharmaceutical Group Co., Ltd |
September 27, 2023 | Phase 3 |
Anti-tremor effect of ACP-103. The number of tremulous jaw movements is shown as a function of ACP-103 dose in combination with tacrine.Pharmacol Biochem Behav.2008 Oct;90(4):540-4. |
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 Anti-dyskinetic effect of ACP-103. Dyskinesia severity score is shown as a function of ACP-103 dose in combination with levodopa in MPTP-treated monkeys.Pharmacol Biochem Behav.2008 Oct;90(4):540-4. |
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