2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Pimavanserin hemitartrate

Pimavanserin hemitartrate  (Synonyms: ACP-103 hemitartrate)

Cat. No.: HY-14557A Purity: 99.91%
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Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

For research use only. We do not sell to patients.

Pimavanserin hemitartrate Chemical Structure

Pimavanserin hemitartrate Chemical Structure

CAS No. : 706782-28-7

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Pimavanserin hemitartrate:

Pimavanserin hemitartrate Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

IC50 & Target

5-HT2A Receptor

8.73 (pIC50)

5-HT2A Receptor

9.3 (pKi)

In Vitro

Pimavanserin hemitartrate competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin hemitartrate displays potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin hemitartrate demonstrates lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and functional activity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pimavanserin hemitartrate Related Antibodies
In Vivo

Pimavanserin hemitartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin hemitartrate demonstrates 42.6% oral bioavailability in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

502.59

Formula

C25H34FN3O2.1/2C4H6O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (198.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (99.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9897 mL 9.9485 mL 19.8969 mL
5 mM 0.3979 mL 1.9897 mL 3.9794 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.91%

COA (251 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Rats: Thirty minutes before being placed in the startle apparatus, rats are treated with saline (s.c.), MDL-100,151 (1.0 mg/kg s.c.), or one of three doses of ACP-103 (1.0, 3.0, or 10.0 mg/kg s.c.). Five minutes after the pretreatment, rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The acoustic startle session lasted approximately 37 min. After 1 week, rats are tested again in the same acoustic/tactile startle session in the exact order and at the same time as the previous week. The same pretreatment drug or vehicle is administered, and rats are crossed over to receive the treatment opposite to that they received the previous week (e.g., DOI HCl for week 1, 0.9% saline for week 2)[1].

Mice: Non-Swiss albino mice are used for locomotor activity experiments. For determination of spontaneous activity, ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min before session start). For hyperactivity experiments, mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peak dose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) in combination with vehicle or ACP-103. Motor activity data are collected during a 15-min session in a lit room[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9897 mL 9.9485 mL 19.8969 mL 49.7423 mL
5 mM 0.3979 mL 1.9897 mL 3.9794 mL 9.9485 mL
10 mM 0.1990 mL 0.9948 mL 1.9897 mL 4.9742 mL
15 mM 0.1326 mL 0.6632 mL 1.3265 mL 3.3162 mL
20 mM 0.0995 mL 0.4974 mL 0.9948 mL 2.4871 mL
25 mM 0.0796 mL 0.3979 mL 0.7959 mL 1.9897 mL
30 mM 0.0663 mL 0.3316 mL 0.6632 mL 1.6581 mL
40 mM 0.0497 mL 0.2487 mL 0.4974 mL 1.2436 mL
50 mM 0.0398 mL 0.1990 mL 0.3979 mL 0.9948 mL
60 mM 0.0332 mL 0.1658 mL 0.3316 mL 0.8290 mL
80 mM 0.0249 mL 0.1244 mL 0.2487 mL 0.6218 mL
DMSO 100 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4974 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Pimavanserin hemitartrate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pimavanserin hemitartrate706782-28-7ACP-103 hemitartrate5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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