KB-R7943 mesylate
new
featured

We are open as normal during COVID-19 pandemic. Order online, same day shipping out from North Carolina, USA

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

MedKoo CAT#: 522400

CAS#: 182004-65-5 (mesylate)

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 Shipping out time Quantity
25mg USD 150 2 Weeks
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 650 2 Weeks
500mg USD 950 2 Weeks
1g USD 1650 2 Weeks
2g USD 2650 2 Weeks
5g USD 3850 2 Weeks
10g USD 4650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

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

img

Theoretical Analysis

MedKoo Cat#: 522400
Name: KB-R7943 mesylate
CAS#: 182004-65-5 (mesylate)
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


Related CAS #: 182004-64-4 (free base)   182004-65-5 (mesylate)    

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 (SDS):

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).

HS Tariff Code:
2934.99.9001


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.