1. Membrane Transporter/Ion Channel
  2. Proton Pump Potassium Channel Na+/K+ ATPase
  3. Tegoprazan

Tegoprazan  (Synonyms: CJ-12420; RQ-00000004)

Cat. No.: HY-17623 Purity: 99.76%
Handling Instructions Technical Support

Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H+/K+-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H+/K+-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases.

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Tegoprazan

Tegoprazan 화학구조

CAS No. : 942195-55-3

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Tegoprazan:

Top Publications Citing Use of Products
  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H+/K+-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H+/K+-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases[1][2][3].

IC50 & Target

IC50: 0.29-0.52 μM (H+/K+-ATPase)[1].

In Vitro

Tegoprazan (1.0 mM and 3.0 mM, 4 h) reduces dextran sulphate sodium (DSS)-induced colitis by maintaining high junction integrity of the epithelial mucosa in Caco-2 cells. Additionally, Tegoprazan protects the intestinal epithelial tight junction barrier and inhibits the increase in intestinal permeability in Caco-2 cells[1].

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

RT-PCR[1]

Cell Line: Caco-2 cells
Concentration: 1.0 mM and 3.0 mM
Incubation Time: 4 h
Result: Increased the mRNA levels of Zo1 and Occludin combined with DSS compared to the DSS+Veh group in Caco-2 cells.
In Vivo

Tegoprazan (30 mg / kg, p.o., twice daily for 5 days) alleviates the severity of dinitrobenzene sulfonic acid (DNBS)-induced reduced colon length and colonic damage, as well as protecting against DNBS-induced colon inflammation in mice colon[1].
Tegoprazan (0.1, 1 and 10 mg/kg, p.o., a single day or daily for 5 days) exerts an antiulcer effect in Naproxen (HY-15030)-induced acute gastric ulcer rat model[2].

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

Animal Model: Naproxen-induced acute gastric ulcer rat model[2].
Dosage: 0.1, 1 and 10 mg/kg
Administration: p.o., a single day or daily for 5 days
Result: Exerted an antiulcer effect in a dose-dependent manner and was effective at a single dose in naproxen-induced acute gastric ulcer rat model.
Animal Model: DNBS and Tegoprazan-induced rats[2].
Dosage: 30 mg/kg
Administration: p.o., twice daily for 5 days
Result: Reduced mRNA expression levels of proinflammatory cytokines, especially interleukin-17 (IL17) in DNBS and Tegoprazan-induced rats.
분자량

387.38

화학식

C20H19F2N3O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC(F)=C2[C@@H](OC3=CC(C(N(C)C)=O)=CC4=C3N=C(C)N4)CCOC2=C1

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 100 mg/mL (258.14 mM; Need ultrasonic; 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 2.5814 mL 12.9072 mL 25.8144 mL
5 mM 0.5163 mL 2.5814 mL 5.1629 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

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: ≥ 2.5 mg/mL (6.45 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 (6.45 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.
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.
순도&문서
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. 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 2.5814 mL 12.9072 mL 25.8144 mL 64.5361 mL
5 mM 0.5163 mL 2.5814 mL 5.1629 mL 12.9072 mL
10 mM 0.2581 mL 1.2907 mL 2.5814 mL 6.4536 mL
15 mM 0.1721 mL 0.8605 mL 1.7210 mL 4.3024 mL
20 mM 0.1291 mL 0.6454 mL 1.2907 mL 3.2268 mL
25 mM 0.1033 mL 0.5163 mL 1.0326 mL 2.5814 mL
30 mM 0.0860 mL 0.4302 mL 0.8605 mL 2.1512 mL
40 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6134 mL
50 mM 0.0516 mL 0.2581 mL 0.5163 mL 1.2907 mL
60 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0756 mL
80 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8067 mL
100 mM 0.0258 mL 0.1291 mL 0.2581 mL 0.6454 mL
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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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상품명:
Tegoprazan
Cat. No.:
HY-17623
수량:
MCE Japan Authorized Agent: