Linaprazan glurate
Based on 1 Customer Validation
Linaprazan glurate (X842) is an orally atcive prodrug of Linaprazan (HY-100412) with a potent and prolonged inhibitory effect on gastric acid secretion. Linaprazan glurate is rapidly transformed by enzymatic cleavage into its active metabolite, linaprazan. Linaprazan glurate is a potassium-competitive acid blocker. Linaprazan glurate selectively inhibites acid formation from gastric H⁺/K⁺-ATPase in a potassium-dependent manner (IC50 = 436.2 nM). Linaprazan glurate can be used for the studies of erosive esophagitis (EE).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.65%
- No. CAS: 1228559-81-6
- Fòrmula: C26H32N4O5
- Peso molecular:480.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
| Species | Dose | Route | Note | T1/2 | Cmax | AUC0-24 |
|---|---|---|---|---|---|---|
| Rat[1] | 0.6 mg/kg | i.v. | male | 0.4 h | 448.1 ng/mL | 145.6 ng·h/mL |
| Rat[1] | 0.6 mg/kg | i.v. | female | 0.4 h | 606.2 ng/mL | 217.8 ng·h/mL |
| Rat[1] | 0.6 mg/kg | p.o. | male | NA h | 2.5 ng/mL | 2.5 ng·h/mL |
| Rat[1] | 0.6 mg/kg | p.o. | female | 2.8 h | 8.7 ng/mL | 13.8 ng·h/mL |
| Rat[1] | 2.4 mg/kg | p.o. | male | 2.6 h | 14.6 ng/mL | 18.3 ng·h/mL |
| Rat[1] | 2.4 mg/kg | p.o. | female | 4.1 h | 42.6 ng/mL | 85.6 ng·h/mL |
| Rat[1] | 9.6 mg/kg | p.o. | male | 2.01 h | 32.0 ng/mL | 134.5 ng·h/mL |
| Rat[1] | 9.6 mg/kg | p.o. | female | 2.1 h | 164.3 ng/mL | 309.8 ng·h/mL |
Linaprazan glurate (2.4 mg/kg, p.o., single dose) is rapidly metabolized in the body, has good target tissue (stomach) selective distribution and low central nervous system permeability, and there are significant gender differences between mice and rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pylorus-ligated model established in Sprague-Dawley rats[1]
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Dosage:0.15, 0.5, 1.0, 1.5 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Reached acid suppression rates by 85%, 61%, and 44% at doses of 1.5, 1.0, and 0.5 mg/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1228559-81-6
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Appearance Solid
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Peso molecular 480.56
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Fòrmula C26H32N4O5
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Color White to off-white
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SMILES
O=C(CCCC(OCCNC(C1=CN2C(C)=C(C)N=C2C(NCC3=C(C)C=CC=C3C)=C1)=O)=O)O
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Synonyms
X842
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 12.5 mg/mL (26.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lu M, et al. Pharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, in vitro and in vivo. Front Pharmacol. 2025 Sep 5;16:1636523. [Content Brief]
[2]. Zhang X, et al. Absorption, distribution, metabolism and excretion of linaprazan glurate in rats. J Pharm Biomed Anal. 2024 May 15;242:116012. [Content Brief]
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. 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 | 1 mM | 2.0809 mL | 10.4045 mL | 20.8091 mL | 52.0226 mL |
| 5 mM | 0.4162 mL | 2.0809 mL | 4.1618 mL | 10.4045 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0809 mL | 5.2023 mL | |
| 15 mM | 0.1387 mL | 0.6936 mL | 1.3873 mL | 3.4682 mL | |
| 20 mM | 0.1040 mL | 0.5202 mL | 1.0405 mL | 2.6011 mL | |
| 25 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0809 mL |
Linaprazan glurate Related Classifications
HY-145578 Related Classifications
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