Cat. No.: HY-12752A

Alimemazine hemitartrate

(Synonyms: Trimeprazine hemitartrate)

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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.

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Pureté: 99.49%
CAS No.: 4330-99-8
Formule: C₁₈H₂₂N₂S.1/2C₄H₆O₆
Masse moléculaire:373.49

Stockage:

4°C, sealed storage, away from moisture

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

Alimemazine hemitartrate Chemical Structure

CAS No.: 4330-99-8

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

GPCR

Voir tous les produits spécifiques à Isoform Histamine Receptor :

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.

Chemical Information

CAS No. 4330-99-8
Appearance Solid
Masse moléculaire 373.49
Formule C₁₈H₂₂N₂S.1/2C₄H₆O₆
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
Synonyms

Trimeprazine hemitartrate
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6774 mL

13.3872 mL

26.7745 mL

5 mM

0.5355 mL

2.6774 mL

5.3549 mL

10 mM

0.2677 mL

1.3387 mL

2.6774 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Singh B, et al. Bioanalytical method development and validation of alimemazine in human plasma by LC-MS/MS and its application in bioequivalence studies. J Pharm Bioallied Sci. 2013 Oct;5(4):257-64. [Content Brief]

[2]. Kuznetsova A, et al. Trimeprazine increases IRS2 in human islets and promotes pancreatic β cell growth and function in mice. JCI Insight. 2016;1(3). [Content Brief]

[3]. Mei Hashizume, et al. Phenothiazines inhibit SARS-CoV-2 cell entry via a blockade of spike protein binding to neuropilin-1. Antiviral Research. Volume 209, January 2023, 105481

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Alimemazine hemitartrate

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Voir tous les produits spécifiques à Isoform Histamine Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Alimemazine hemitartrate Related Classifications

HY-12752A Related Classifications