2. Membrane Transporter/Ion Channel
  3. Proton Pump
  4. SCH28080

SCH28080 est un inhibiteur de la gastrique(H+/K+)-ATPase qui est K+-competitive et réversible, avec unKi de 0,12 μM. SCH28080 est un inhibiteur efficace de la sécrétion d'acide in vivo et avec une activité anti-ulcère gastrique.

SCH28080 is a reversible, K+-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.

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

SCH28080 Chemical Structure

SCH28080 Chemical Structure

CAS No. : 76081-98-6

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Based on 1 publication(s) in Google Scholar

SCH28080 Related Antibodies

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Description

SCH28080 is a reversible, K+-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity[1][2][3].

IC50 & Target

Ki: 0.12 μM ((H+/K+)-ATPase)[1]
In Vitro

SCH28080 competitively inhibits the K+-stimulated hydrolysis of ATP, with a Ki of 0.12 μM [1].
SCH28080 inhibits histamine-induced [14C]aminopyrine uptake into isolated rabbit parietal cells with an IC50 of 0.029 μM[1].
SCH28080 causes a dose-dependent reduction in cell viability with IC50 values of 22.9 μM and 15.3 μM after 2 h and 24 h treatments, respectively, and cell viability was below 10% at 100 μM already after 2 h treatment[2].
SCH28080 induces apoptosis and is cytotoxic at higher doses[2].
SCH28080 inhibits insulin secretion by activation of IK ATP and inhibition of L-type voltage-gated Ca2+ channels, reduces cell viability and dose-dependently induces apoptosis/necrosis[2].

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

SCH28080 Related Antibodies

Cell Viability Assay[2]

Cell Line: INS-1E cell
Concentration: 3.1 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 2 hours, 24 hours
Result: Caused a dose-dependent reduction in cell viability.
In Vivo

SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats[3].

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

Animal Model: Male Wistar rat (280-350 g), the Shay rat model[3]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection
Result: Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.
Molecular Weight

277.32

Formula

C17H15N3O
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (360.59 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 3.6059 mL 18.0297 mL 36.0594 mL
5 mM 0.7212 mL 3.6059 mL 7.2119 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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 (9.01 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 (9.01 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.
Purity & Documentation

Purity: ≥99.0%

SDS (393 KB)

COA (250 KB)

Handling Instructions (2659 KB)
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 3.6059 mL 18.0297 mL 36.0594 mL 90.1486 mL
5 mM 0.7212 mL 3.6059 mL 7.2119 mL 18.0297 mL
10 mM 0.3606 mL 1.8030 mL 3.6059 mL 9.0149 mL
15 mM 0.2404 mL 1.2020 mL 2.4040 mL 6.0099 mL
20 mM 0.1803 mL 0.9015 mL 1.8030 mL 4.5074 mL
25 mM 0.1442 mL 0.7212 mL 1.4424 mL 3.6059 mL
30 mM 0.1202 mL 0.6010 mL 1.2020 mL 3.0050 mL
40 mM 0.0901 mL 0.4507 mL 0.9015 mL 2.2537 mL
50 mM 0.0721 mL 0.3606 mL 0.7212 mL 1.8030 mL
60 mM 0.0601 mL 0.3005 mL 0.6010 mL 1.5025 mL
80 mM 0.0451 mL 0.2254 mL 0.4507 mL 1.1269 mL
100 mM 0.0361 mL 0.1803 mL 0.3606 mL 0.9015 mL
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SCH28080 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.

Keywords:

SCH2808076081-98-6SCH 28080SCH-28080Proton Pumpgastriculcer(H++K+)-ATPase(H+/K+)-ATPaseanti-gastricinsulinsecretionanti-ulcerInhibitorinhibitorinhibit

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