KB-R7943 mesylate
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MedKoo CAT#: 522400

CAS#: 182004-65-5

Description: KB-R7943 is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 μM). KB-R7943 does not modify secondary pathology in the thalamus following focal cerebral stroke in rats. KB-R7943 blocks opening of the mitochondrial permeability transition pore. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion.


Price and Availability

Size
Price

25mg
USD 150
200mg
USD 650
2g
USD 2650
Size
Price

50mg
USD 250
500mg
USD 950
5g
USD 3850
Size
Price

100mg
USD 450
1g
USD 1650
10g
USD 4650

KB-R7943 mesylate, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2.0g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522400
Name: KB-R7943 mesylate
CAS#: 182004-65-5
Chemical Formula: C17H21N3O6S2
Exact Mass: 427.08718
Molecular Weight: 427.49
Elemental Analysis: C, 47.76; H, 4.95; N, 9.83; O, 22.46; S, 15.00


Synonym: KB-R7943; KB R7943; KB-R 7943; KB-R7943 mesylate

IUPAC/Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate

InChi Key: WGIKEBHIKKWJLG-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4)

SMILES Code: N=C(N)SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1.OS(=O)(C)=O


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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, not in water

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).

Harmonized System Code:
293490


References

1: Chang PC, Wo HT, Lee HL, Wen MS, Chou CC. Paradoxical effects of KB-R7943 on arrhythmogenicity in a chronic myocardial infarction rabbit model. J Cardiol. 2015 Jul;66(1):80-7. doi: 10.1016/j.jjcc.2014.08.002. Epub 2014 Sep 16. PubMed PMID: 25241015.

2: Lipsanen A, Parkkinen S, Khabbal J, Mäkinen P, Peräniemi S, Hiltunen M, Jolkkonen J. KB-R7943, an inhibitor of the reverse Na(+)/Ca(2+) exchanger, does not modify secondary pathology in the thalamus following focal cerebral stroke in rats. Neurosci Lett. 2014 Sep 19;580:173-7. doi: 10.1016/j.neulet.2014.08.003. Epub 2014 Aug 12. PubMed PMID: 25123443.

3: Abramochkin DV, Vornanen M. Inhibition of the cardiac ATP-dependent potassium current by KB-R7943. Comp Biochem Physiol A Mol Integr Physiol. 2014 Sep;175:38-45. doi: 10.1016/j.cbpa.2014.05.005. Epub 2014 May 17. PubMed PMID: 24845199.

4: Ren Y, Deng L, Cai Y, Lv Y, Jia D. The protective effect of Na+/Ca2+ exchange blocker kb-r7943 on myocardial ischemia-reperfusion injury in hypercholesterolemic rat. Cell Biochem Biophys. 2014 Nov;70(2):1017-22. doi: 10.1007/s12013-014-0012-7. PubMed PMID: 24840224.

5: Re: Yamashita J, Itoh M, Kuro T, Kobayashi Y, Ogata M, Takaoka m, and Matsumura Y (2001) pre- or post-ischemic treatment with a novel na+/ca2+ exchange inhibitor, kb-r7943, shows renal protective effects in rats with ischemic acute renal failure. J pharmacol exp ther 296:412-419. J Pharmacol Exp Ther. 2014 May;349(2):344. doi: 10.1124/jpet.114.05er14. PubMed PMID: 24713231.

6: Wiczer BM, Marcu R, Hawkins BJ. KB-R7943, a plasma membrane Na(+)/Ca(2+) exchanger inhibitor, blocks opening of the mitochondrial permeability transition pore. Biochem Biophys Res Commun. 2014 Jan 31;444(1):44-9. doi: 10.1016/j.bbrc.2014.01.009. Epub 2014 Jan 14. PubMed PMID: 24434143; PubMed Central PMCID: PMC3951502.

7: Abramochkin DV, Alekseeva EI, Vornanen M. Inhibition of the cardiac inward rectifier potassium currents by KB-R7943. Comp Biochem Physiol C Toxicol Pharmacol. 2013 Sep;158(3):181-6. doi: 10.1016/j.cbpc.2013.08.001. Epub 2013 Aug 22. PubMed PMID: 23973826.

8: Yang D, Yang D, Jia R, Tan J. Na+/Ca2+ exchange inhibitor, KB-R7943, attenuates contrast-induced acute 
kidney injury. J Nephrol. 2013 Sep-Oct;26(5):877-85. doi: 10.5301/jn.5000259. Epub 2013 Mar 5. PubMed PMID: 23475466.

9: Lv Y, Ren Y, Sun L, Wang S, Wei M, Jia D. Protective effect of Na(+)/Ca (2+) exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in hypercholesterolemic rats. Cell Biochem Biophys. 2013 Jun;66(2):357-63. doi: 10.1007/s12013-012-9474-7. PubMed PMID: 23212178.

10: Su Y, Mao N, Li M, Dong X, Lin FZ, Xu Y, Li YB. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. J Diabetes Complications. 2013 Jan-Feb;27(1):6-10. doi: 10.1016/j.jdiacomp.2012.08.007. Epub 2012 Sep 27. PubMed PMID: 23021774.

11: Ren Y, Cai Y, Jia D. Comparative antiapoptotic effects of KB-R7943 and ischemic postconditioning during myocardial ischemia reperfusion. Cell Biochem Biophys. 2012 Nov;64(2):137-45. doi: 10.1007/s12013-012-9382-x. PubMed PMID: 22707298.

12: Cheng H, Zhang Y, Du C, Dempsey CE, Hancox JC. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol. 2012 Apr;165(7):2260-73. doi: 10.1111/j.1476-5381.2011.01688.x. PubMed PMID: 21950687; PubMed Central PMCID: PMC3413861.

13: Cheng H, Smith GL, Hancox JC, Orchard CH. Inhibition of spontaneous activity of rabbit atrioventricular node cells by KB-R7943 and inhibitors of sarcoplasmic reticulum Ca(2+) ATPase. Cell Calcium. 2011 Jan;49(1):56-65. doi: 10.1016/j.ceca.2010.11.008. Epub 2010 Dec 15. PubMed PMID: 21163524; PubMed Central PMCID: PMC3048929.

14: Jia D. The protective effect of mitochondrial ATP-sensitive K+ channel opener, nicorandil, combined with Na+/Ca2+ exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in rat. Cell Biochem Biophys. 2011 Jul;60(3):219-24. doi: 10.1007/s12013-010-9142-8. PubMed PMID: 21132540.

15: Brustovetsky T, Brittain MK, Sheets PL, Cummins TR, Pinelis V, Brustovetsky N. KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br J Pharmacol. 2011 Jan;162(1):255-70. doi: 10.1111/j.1476-5381.2010.01054.x. PubMed PMID: 20883473; PubMed Central PMCID: PMC3012420.

16: Tashiro M, Inoue H, Konishi M. KB-R7943 inhibits Na+-dependent Mg2+ efflux in rat ventricular myocytes. J Physiol Sci. 2010 Nov;60(6):415-24. doi: 10.1007/s12576-010-0113-z. Epub 2010 Sep 23. PubMed PMID: 20862573.

17: Algara-Suárez P, Mejía-Elizondo R, Sims SM, Saavedra-Alanis VM, Espinosa-Tanguma R. The 1.3 isoform of Na+-Ca 2+ exchanger expressed in guinea pig tracheal smooth muscle is less sensitive to KB-R7943. J Physiol Biochem. 2010 Jun;66(2):117-25. doi: 10.1007/s13105-010-0016-8. Epub 2010 Apr 29. PubMed PMID: 20428991.

18: Condrescu M, Reeves JP. Inhibition of sodium-calcium exchange by KB-R7943: Dodecylamine and sphingosine in transfected Chinese hamster ovary cells. Cell Calcium. 2010 May;47(5):404-11. doi: 10.1016/j.ceca.2010.02.004. Epub 2010 Mar 5. PubMed PMID: 20206994.

19: Li J, Jin HB, Sun YM, Su Y, Wang LF. KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion. Biochem Biophys Res Commun. 2010 Feb 19;392(4):516-9. doi: 10.1016/j.bbrc.2009.12.183. Epub 2010 Jan 22. PubMed PMID: 20096662.

20: Storozhevykh TP, Senilova YE, Brustovetsky T, Pinelis VG, Brustovetsky N. Neuroprotective effect of KB-R7943 against glutamate excitotoxicity is related to mild mitochondrial depolarization. Neurochem Res. 2010 Feb;35(2):323-35. doi: 10.1007/s11064-009-0058-x. Epub 2009 Sep 22. PubMed PMID: 19771515.