SCH28080

CAS No. 76081-98-6

SCH28080( —— )

Catalog No. M21900 CAS No. 76081-98-6

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    SCH28080
  • Note
    Research use only, not for human use.
  • Brief 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.
  • 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.
  • In Vitro
    SCH28080 competitively inhibits the K+-stimulated hydrolysis of ATP, with a Ki of 0.12 μM .SCH28080 inhibits histamine-induced [14C]aminopyrine uptake into isolated rabbit parietalcells with an IC50 of 0.029 μM.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.SCH28080 induces apoptosis and is cytotoxic at higher doses.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. Cell Viability Assay 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. Animal Model:Male Wistar rat (280-350 g), the Shay rat modelDosage:20 mg/kg Administration:Intraperitoneal injection Result:Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    Proton Pump
  • Recptor
    Ki: 0.12μM ((H+/K+)-ATPase)
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    76081-98-6
  • Formula Weight
    277.32
  • Molecular Formula
    C??H??N?O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (360.59 mM)
  • SMILES
    N#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Scott CK, et al. Studies on the mechanism of action of the gastric microsomal (H+ + K+)-ATPase inhibitors SCH 32651 and SCH 28080. Biochem Pharmacol. 1987 Jan 1;36(1):97-104. 2. Martin Jakab, et al. The H+/K+ ATPase Inhibitor SCH-28080 Inhibits Insulin Secretion and Induces Cell Death in INS-1E Rat Insulinoma Cells. Cell Physiol Biochem. 2017;43(3):1037-1051. 3. Y Hamagishi, et al. Inhibitory Effects of Copiamycin A, a Macrocyclic Lactone Antibiotic, on Gastric H+,K(+)-ATPase, Acid Secretion and Ulcer Formation. Jpn J Pharmacol. 1991 Feb;55(2):283-6.
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