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

SCH28080 

Cat. No.: HY-103261 Purity: >99.0%
Handling Instructions

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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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: 0.12μM ((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 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].

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].

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.

76081-98-6

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
References

Purity: >99.0%

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Keywords:

SCH28080SCH 28080SCH-28080Proton Pumpgastriculcer(H++K+)-ATPase(H+/K+)-ATPaseanti-gastricinsulinsecretionanti-ulcerInhibitorinhibitorinhibit

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SCH28080
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