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Linaprazan  (Synonyms: AZD0865)

Cat. No.: HY-100412 Purity: 99.61%
COA Handling Instructions

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding.

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

Linaprazan Chemical Structure

Linaprazan Chemical Structure

CAS No. : 248919-64-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 450 In-stock
100 mg USD 700 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. In vitro: Linaprazan can inhibit the final step in acid secretion. Linaprazanreduced porcine renal Na+,K+-ATPase activity by 9 ± 2%, demonstrating a high selectivity for H+,K+-ATPase. In vivo: The reference for animal administration is 0.5-1.0 mg/kg. The greater degree of acid suppression with the 75-mg dose of Linaprazan would translate to a healing rate of 89% at 4 weeks.

Clinical Trial
Molecular Weight

366.46

Formula

C21H26N4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN2C(C(NCC3=C(C)C=CC=C3C)=C1)=NC(C)=C2C)NCCO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (95.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7288 mL 13.6441 mL 27.2881 mL
5 mM 0.5458 mL 2.7288 mL 5.4576 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (5.68 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.61%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7288 mL 13.6441 mL 27.2881 mL 68.2203 mL
5 mM 0.5458 mL 2.7288 mL 5.4576 mL 13.6441 mL
10 mM 0.2729 mL 1.3644 mL 2.7288 mL 6.8220 mL
15 mM 0.1819 mL 0.9096 mL 1.8192 mL 4.5480 mL
20 mM 0.1364 mL 0.6822 mL 1.3644 mL 3.4110 mL
25 mM 0.1092 mL 0.5458 mL 1.0915 mL 2.7288 mL
30 mM 0.0910 mL 0.4548 mL 0.9096 mL 2.2740 mL
40 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7055 mL
50 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3644 mL
60 mM 0.0455 mL 0.2274 mL 0.4548 mL 1.1370 mL
80 mM 0.0341 mL 0.1706 mL 0.3411 mL 0.8528 mL
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Linaprazan Related Classifications

Help & FAQs
  • 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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Linaprazan
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