SCH 28080 | CAS#76081-98-6 | gastric H+ and K+-ATPase inhibitor

MedKoo Cat#: 526288 | Name: SCH 28080

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SCH 28080 is a potent inhibitor of gastric H+ and K+-ATPase. SCH- 28080 inhibits the isolated enzyme activity with a potency similar to omeprazole, IC50s of 2.5 and 4.0 μM respectively.

Chemical Structure

SCH 28080

CAS#76081-98-6

Theoretical Analysis

MedKoo Cat#: 526288

Name: SCH 28080

CAS#: 76081-98-6

Chemical Formula: C17H15N3O

Exact Mass: 277.1215

Molecular Weight: 277.32

Elemental Analysis: C, 73.63; H, 5.45; N, 15.15; O, 5.77

Price and Availability

Size	Price	Availability
5mg	USD 250.00	2 Weeks
10mg	USD 450.00	2 Weeks
50mg	USD 1,150.00	2 Weeks

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Related CAS #

No Data

Synonym

SCH 28080; SCH28080; SCH-28080.

IUPAC/Chemical Name

Imidazo(1,2-a)pyridine-3-acetonitrile, 2-methyl-8-(phenylmethoxy)-

InChi Key

InChi Code

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Biological target:

Ki: 0.12 μM ((H+/K+)-ATPase)

In vitro activity:

The effects of three specific H+/K+-ATPase inhibitors (omeprazole, lansoprazole and SCH 28080) were investigated on the mechanical and electrophysiological properties of rat atrium, in vitro. Reference: Yenisehirli A, Onur R. Positive inotropic and negative chronotropic effects of proton pump inhibitors in isolated rat atrium. Eur J Pharmacol. 2005 Sep 20;519(3):259-66. doi: 10.1016/j.ejphar.2005.06.040. PMID: 16125697.

In vivo activity:

The Na+-dependent K+-ATPase accounted for approximately 80% of overall K+-ATPase activity and was characterized by insensitivity to Sch-28080 but partial sensitivity to ouabain. Reference: Codina J, Pressley TA, DuBose TD Jr. The colonic H+,K+-ATPase functions as a Na+-dependent K+(NH4+)-ATPase in apical membranes from rat distal colon. J Biol Chem. 1999 Jul 9;274(28):19693-8. doi: 10.1074/jbc.274.28.19693. PMID: 10391909.

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	360.59

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 277.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

In vitro protocol:

1: Yenisehirli A, Onur R. Positive inotropic and negative chronotropic effects of proton pump inhibitors in isolated rat atrium. Eur J Pharmacol. 2005 Sep 20;519(3):259-66. doi: 10.1016/j.ejphar.2005.06.040. PMID: 16125697. 2: Munson K, Lambrecht N, Shin JM, Sachs G. Analysis of the membrane domain of the gastric H(+)/K(+)-ATPase. J Exp Biol. 2000 Jan;203(Pt 1):161-70. doi: 10.1242/jeb.203.1.161. PMID: 10600685.

In vivo protocol:

1: Codina J, Pressley TA, DuBose TD Jr. The colonic H+,K+-ATPase functions as a Na+-dependent K+(NH4+)-ATPase in apical membranes from rat distal colon. J Biol Chem. 1999 Jul 9;274(28):19693-8. doi: 10.1074/jbc.274.28.19693. PMID: 10391909. 2: Khanna A, Simoni J, Wesson DE. Endothelin-induced increased aldosterone activity mediates augmented distal nephron acidification as a result of dietary protein. J Am Soc Nephrol. 2005 Jul;16(7):1929-35. doi: 10.1681/ASN.2004121054. Epub 2005 May 4. PMID: 15872074.

1: Laroche-Joubert N, Marsy S, Doucet A. Cellular origin and hormonal regulation of K(+)-ATPase activities sensitive to Sch-28080 in rat collecting duct. Am J Physiol Renal Physiol. 2000 Dec;279(6):F1053-9. PubMed PMID: 11097623. 2: Farley RA, Schreiber S, Wang SG, Scheiner-Bobis G. A hybrid between Na+,K+-ATPase and H+,K+-ATPase is sensitive to palytoxin, ouabain, and SCH 28080. J Biol Chem. 2001 Jan 26;276(4):2608-15. PubMed PMID: 11054424. 3: Codina J, Cardwell J, Gitomer JJ, Cui Y, Kone BC, Dubose TD Jr. Sch-28080 depletes intracellular ATP selectively in mIMCD-3 cells. Am J Physiol Cell Physiol. 2000 Nov;279(5):C1319-26. PubMed PMID: 11029278. 4: Rhoden KJ. Inhibition of vascular smooth muscle tone by the H+, K+-ATPase inhibitor SCH 28080. J Pharm Pharmacol. 2000 Jul;52(7):857-62. PubMed PMID: 10933137. 5: Rulli SJ, Horiba MN, Skripnikova E, Rabon EC. Glu-857 moderates K+-dependent stimulation and SCH 28080-dependent inhibition of the gastric H,K-ATPase. J Biol Chem. 1999 May 21;274(21):15245-50. PubMed PMID: 10329734. 6: Asano S, Matsuda S, Hoshina S, Sakamoto S, Takeguchi N. A chimeric gastric H+,K+-ATPase inhibitable with both ouabain and SCH 28080. J Biol Chem. 1999 Mar 12;274(11):6848-54. PubMed PMID: 10066737. 7: Swarts HG, Hermsen HP, Koenderink JB, Willems PH, de Pont JJ. Conformation-dependent inhibition of gastric H+,K+-ATPase by SCH 28080 demonstrated by mutagenesis of glutamic acid 820. Mol Pharmacol. 1999 Mar;55(3):541-7. PubMed PMID: 10051539. 8: Wall SM, Mehta P, DuBose TD Jr. Dietary K+ restriction upregulates total and Sch-28080-sensitive bicarbonate absorption in rat tIMCD. Am J Physiol. 1998 Oct;275(4 Pt 2):F543-9. PubMed PMID: 9755126. 9: Swarts HP, Klaassen CH, De Pont JJ. Involvement of glutamic acid 820 in K+ and SCH 28080 binding to gastric H+,K(+)-ATPase. Ann N Y Acad Sci. 1997 Nov 3;834:472-4. PubMed PMID: 9405848. 10: Asano S, Matsuda S, Tega Y, Shimizu K, Sakamoto S, Takeguchi N. Mutational analysis of putative SCH 28080 binding sites of the gastric H+,K+-ATPase. J Biol Chem. 1997 Jul 11;272(28):17668-74. PubMed PMID: 9211917. 11: Lyu RM, Farley RA. Amino acids Val115-Ile126 of rat gastric H(+)-K(+)-ATPase confer high affinity for Sch-28080 to Na(+)-K(+)-ATPase. Am J Physiol. 1997 May;272(5 Pt 1):C1717-25. PubMed PMID: 9176164. 12: Javaheri S, Corbett WS, Simbartl LA, Mehta S, Khosla A. Different effects of omeprazole and Sch 28080 on canine cerebrospinal fluid production. Brain Res. 1997 Apr 18;754(1-2):321-4. PubMed PMID: 9134992. 13: Buffin-Meyer B, Younes-Ibrahim M, Barlet-Bas C, Cheval L, Marsy S, Doucet A. K depletion modifies the properties of Sch-28080-sensitive K-ATPase in rat collecting duct. Am J Physiol. 1997 Jan;272(1 Pt 2):F124-31. PubMed PMID: 9039058. 14: Zhou X, Wingo CS. Stimulation of total CO2 flux by 10% CO2 in rabbit CCD: role of an apical Sch-28080- and Ba-sensitive mechanism. Am J Physiol. 1994 Jul;267(1 Pt 2):F114-20. PubMed PMID: 8048550. 15: Sabolić I, Brown D, Verbavatz JM, Kleinman J. H(+)-ATPases of renal cortical and medullary endosomes are differentially sensitive to Sch-28080 and omeprazole. Am J Physiol. 1994 Jun;266(6 Pt 2):F868-77. PubMed PMID: 7517642. 16: Graber ML, Devine P. Omeprazole and SCH 28080 inhibit acid secretion by the turtle urinary bladder. Ren Physiol Biochem. 1993 Sep-Oct;16(5):257-67. PubMed PMID: 7694339. 17: Kohn OF, Mitchell PP, Steinmetz PR. Sch-28080 inhibits bafilomycin-sensitive H+ secretion in turtle bladder independently of luminal [K+]. Am J Physiol. 1993 Aug;265(2 Pt 2):F174-9. PubMed PMID: 8368331. 18: Nagaya H, Satoh H. [Possible mechanisms for (H+ + K+)-ATPase inhibition by proton pump inhibitors, omeprazole, lansoprazole and SCH 28080]. Nihon Rinsho. 1992 Jan;50(1):26-32. Japanese. PubMed PMID: 1311786. 19: Van der Hijden HT, Koster HP, Swarts HG, De Pont JJ. Phosphorylation of H+/K(+)-ATPase by inorganic phosphate. The role of K+ and SCH 28080. Biochim Biophys Acta. 1991 Jan 30;1061(2):141-8. PubMed PMID: 1847826. 20: Helander HF, Mattsson H, Elm G, Ottosson S. Structure and function of rat parietal cells during treatment with omeprazole, SCH 28080, SCH 32651, or ranitidine. Scand J Gastroenterol. 1990 Aug;25(8):799-809. PubMed PMID: 2169644.