1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Anti-infection
  2. Histamine Receptor Influenza Virus
  3. Alimemazine hemitartrate

Alimemazine hemitartrate  (Synonyms: Trimeprazine hemitartrate)

Cat. No.: HY-12752A Purity: 98.44%
COA Handling Instructions

Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice.

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

Alimemazine hemitartrate Chemical Structure

Alimemazine hemitartrate Chemical Structure

CAS No. : 4330-99-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
25 mg USD 50 In-stock
50 mg USD 80 In-stock
100 mg USD 120 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice[1][2][3].

IC50 & Target

GPCR

 

In Vitro

Alimemazine hemitartrate (20 μg/mL, 24 h) promotes CREB phosphorylation and increases the concentration of insulin receptor substrate 2 (IRS2)[2].
Alimemazine hemitartrate (20 mg/L) antagonizes GPCR by inhibiting homologous agonists[2].
Alimemazine hemitartrate (10 μM, 90 min) reduces the formation of syncytia induced by SARS-CoV-2 and its variants[3].
Alimemazine hemitartrate (10 μM, 90 min) inhibits SARS-CoV-2 in HEK293T/ACE2 and VeroE6/TMPRSS2 cells[3].

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

Western Blot Analysis[2]

Cell Line: Isolated human islets
Concentration: 20 μg/mL
Incubation Time: 24 h
Result: Increased CREB phosphorylation and IRS2 expression in human pancreatic islets.

Real Time qPCR[2]

Cell Line: Isolated human islets
Concentration: 20 μg/mL
Incubation Time: 5 h
Result: Increased expression of IRS2, FOXO1, and FOXO3A, and decreased expression of PDX1 and GLUT2.

Immunofluorescence[3]

Cell Line: HEK293T/ACE2
Concentration: 10 μg/mL
Incubation Time: 90 min
Result: Reduced syncytia formation induced by SARS2-S and SARS2-S mutants.
In Vivo

Alimemazine hemitartrate (10 mg/kg, intraperitoneal injection, once a day for 3 weeks) promotes mouse β-cell growth[2].
Alimemazine hemitartrate (10 mg/kg, intraperitoneal injection, once a day for 22 days) synergistically reduces the progression of diabetes in NOD mice[2].
Alimemazine hemitartrate (10 mg/kg, intraperitoneal injection, once a day for 7 days) promotes the proliferation and survival of β-cells in normal mice, but has little effect on β-cell defects caused by IRS2 deficiency[2].
Alimemazine hemitartrate (10 mg/kg, oral gavage, two doses) does not reduce mouse lung virus titers[3].

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

Animal Model: Pdx1+/– mice[2]
Dosage: 10 mg/kg, once a day for 3 weeks
Administration: Intraperitoneal injection (i.p.)
Result: Increased HOMA 2%B and normalized glucose tolerance in mice.
Animal Model: Irs2-/–mice[2]
Dosage: 10 mg/kg, once a day for seven days
Administration: Intraperitoneal injection (i.p.)
Result: Did not restore the function of β cells, but promoted β cell growth and increased the area of β cells in normal mice.
Increased the concentration of IRS2 protein, had no effect on glucose tolerance in mice, and did not change the insulin sensitivity of mice.
Animal Model: SARS-CoV-2 multiplication in mice[3]
Dosage: 10mg/kg, at 1 h prior to and 24 h after virus inoculation
Administration: i.g.
Result: Did not reduce lung virus titers.
Molecular Weight

373.49

Formula

C18H22N2S.1/2C4H6O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(CN(C)C)CN1C2=CC=CC=C2SC3=CC=CC=C13.O=C(O)[C@H](O)[C@@H](O)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (267.74 mM; Need ultrasonic)

DMSO : 30 mg/mL (80.32 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6774 mL 13.3872 mL 26.7745 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (133.87 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.6774 mL 13.3872 mL 26.7745 mL 66.9362 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 mL 13.3872 mL
10 mM 0.2677 mL 1.3387 mL 2.6774 mL 6.6936 mL
15 mM 0.1785 mL 0.8925 mL 1.7850 mL 4.4624 mL
20 mM 0.1339 mL 0.6694 mL 1.3387 mL 3.3468 mL
25 mM 0.1071 mL 0.5355 mL 1.0710 mL 2.6774 mL
30 mM 0.0892 mL 0.4462 mL 0.8925 mL 2.2312 mL
40 mM 0.0669 mL 0.3347 mL 0.6694 mL 1.6734 mL
50 mM 0.0535 mL 0.2677 mL 0.5355 mL 1.3387 mL
60 mM 0.0446 mL 0.2231 mL 0.4462 mL 1.1156 mL
80 mM 0.0335 mL 0.1673 mL 0.3347 mL 0.8367 mL
H2O 100 mM 0.0268 mL 0.1339 mL 0.2677 mL 0.6694 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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  • 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.

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Alimemazine hemitartrate
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