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Alizapride HCl

Alias: MS 5080; MS5080; Limican; Plitican; Vergentan; Superan; Alizaprida; Litican; MS-5080
Cat No.:V1255 Purity: ≥98%
Alizapride HCl (Limican; Plitican; Vergentan; Superan; Alizaprida; Litican; MS-5080), the hydrochloride salt of alizapride which is a medication used for the theropy of nausea and vomiting, is a potent dopamine receptor antagonist with prokinetic and antiemetic effects.
Alizapride HCl
Alizapride HCl Chemical Structure CAS No.: 59338-87-3
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
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Other Forms of Alizapride HCl:

  • Alizapride
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Alizapride HCl (Limican; Plitican; Vergentan; Superan; Alizaprida; Litican; MS-5080), the hydrochloride salt of alizapride which is a medication used for the theropy of nausea and vomiting, is a potent dopamine receptor antagonist with prokinetic and antiemetic effects.

Biological Activity I Assay Protocols (From Reference)
Targets
Dopamine receptor
ln Vitro

In vitro activity: Alizapride has an N-allyl moiety, which means it may go through epoxidation, N-deallylation, or other reactions that lead to the formation of chemically reactive metabolites.[1]

ln Vivo
Alizapride shows little toxicity (especially when administered parenterally) in mice and rats. In rodents and mice, alipride exhibits minimal toxicity (particularly when given topically). When administered orally or intravenously, Alizapride is primarily eliminated as an unchanged medication; however, approximately 25% of the drug goes through metabolic conversion prior to elimination. In rats, the aforementioned doses of apomorphine cause a decrease in gastrointestinal transit, which is counteracted by alisparid (5 mg/kg, s.c.).[2]
Enzyme Assay
A dopamine receptor antagonist with prokinetic and antiemetic properties, alizapride hydrochloride is also used to treat nausea and vomiting, including postoperative nausea and vomiting.
Animal Protocol
Male Duncan–Hartley guinea pigs
Dosage: 2.5, 5, 10, 25 μg/kg
Administration: Alizapride (2.5, 5, 10, 25 μg/kg; SC; 7 consecutive days)
References

[1]. Activity of a new antiemetic agent: alizapride. A randomized double-blind crossover controlled trial. Cancer Chemother Pharmacol. 1988;22(4):316-20..

Additional Infomation
Alizapride Hydrochloride is the hydrochloride salt form of alizapride, a methoxy-2-benzamide derivative and dopamine 2 (D2) receptor antagonist, with antiemetic activity. Upon administration, alizapride binds to and blocks the D2 receptor in the chemoreceptive trigger zone (CTZ) of the medulla, thereby preventing nausea and vomiting.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H22CLN5O2
Molecular Weight
351.83
Exact Mass
351.146
Elemental Analysis
C, 54.62; H, 6.30; Cl, 10.08; N, 19.91; O, 9.09
CAS #
59338-87-3
Related CAS #
Alizapride; 59338-93-1; Alizapride-13C,d3 hydrochloride
PubChem CID
135497066
Appearance
Solid powder
Density
1.224 g/cm3
Boiling Point
580.3ºC at 760 mmHg
Melting Point
206-208°
Flash Point
304.8ºC
LogP
2.477
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
6
Heavy Atom Count
24
Complexity
433
Defined Atom Stereocenter Count
0
InChi Key
BRECEDGYMYXGNF-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H21N5O2.ClH/c1-3-6-21-7-4-5-11(21)10-17-16(22)12-8-13-14(19-20-18-13)9-15(12)23-2;/h3,8-9,11H,1,4-7,10H2,2H3,(H,17,22)(H,18,19,20);1H
Chemical Name
6-methoxy-N-[(1-prop-2-enylpyrrolidin-2-yl)methyl]-3H-benzotriazole-5-carboxamide;hydrochloride
Synonyms
MS 5080; MS5080; Limican; Plitican; Vergentan; Superan; Alizaprida; Litican; MS-5080
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: 33.3~42 mg/mL (94.7~119.4 mM)
Water: ~70 mg/mL (~198.95 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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 25.0 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: ≥ 2.5 mg/mL (7.11 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 50 mg/mL (142.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8423 mL 14.2114 mL 28.4228 mL
5 mM 0.5685 mL 2.8423 mL 5.6846 mL
10 mM 0.2842 mL 1.4211 mL 2.8423 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

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