WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H556225
CAS#: 474960-44-6
Description: SB 657510 is a selective urotensin-II (UT) receptor antagonist. SB-657510 inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50 - 189 nM). SB-657510 dramatically blocked the UII-induced increase in adhesion between U937 and EA.hy926 cells. In addition, SB-657510 remarkably reduced UII-induced expression of TF in EA.hy926 cells. Taken together, our results demonstrate that the UII antagonist SB-657510 decreases the progression of inflammation induced by UII in endothelial cells.
Hodoodo Cat#: H556225
Name: SB-657510
CAS#: 474960-44-6
Chemical Formula: C19H22BrClN2O5S
Exact Mass: 504.01
Molecular Weight: 505.808
Elemental Analysis: C, 45.12; H, 4.38; Br, 15.80; Cl, 7.01; N, 5.54; O, 15.82; S, 6.34
Synonym: SB-657510; SB 657510; SB657510;
IUPAC/Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
InChi Key:
InChi Code:
SMILES Code: O=S(C1=CC(OC)=C(OC)C=C1Br)(NC2=CC=C(Cl)C(O[C@H]3CN(C)CC3)=C2)=O
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 505.81 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: | |
| In vivo protocol: |
1: Li J, Zhao PP, Hao T, Wang D, Wang Y, Zhu YZ, Wu YQ, Zhou CH. Urotensin II inhibitor eases neuropathic pain by suppressing the JNK/NF-κB pathway. J Endocrinol. 2017 Feb;232(2):165-174. doi: 10.1530/JOE-16-0255. PMID: 27895138.
2: Chen GJ, Wu F, Pang XX, Zhang AH, Shi JB, Lu M, Tang CS. Retraction statement: ‘Urotensin II inhibits autophagy in renal tubular epithelial cells and induces extracellular matrix production in early diabetic mice’ by Guan‐Jong Chen, Fei Wu, Xin‐Xin Pang, Ai‐Hua Zhang, Jun‐Bao Shi, Min Lu and Chao‐Shu Tang. J Diabetes Investig. 2017 Jul;8(4):629. doi: 10.1111/jdi.12557. Epub 2016 Jul 26. PMID: 27459313; PMCID: PMC5497045.
3: Goldberg AA, Joung KB, Mansuri A, Kang Y, Echavarria R, Nikolajev L, Sun Y, Yu JJ, Laporte SA, Schwertani A, Kristof AS. Oncogenic effects of urotensin-II in cells lacking tuberous sclerosis complex-2. Oncotarget. 2016 Sep 20;7(38):61152-61165. doi: 10.18632/oncotarget.10748. PMID: 27458154; PMCID: PMC5308642.
4: Palabiyik SS, Karakus E, Akpinar E, Halici Z, Bayir Y, Yayla M, Kose D. The Role of Urotensin Receptors in the Paracetamol-Induced Hepatotoxicity Model in Mice: Ameliorative Potential of Urotensin II Antagonist. Basic Clin Pharmacol Toxicol. 2016 Feb;118(2):150-9. doi: 10.1111/bcpt.12447. Epub 2015 Aug 13. PMID: 26176337.
5: Mueller LE, Kausch MA, Markovic T, MacLaren DA, Dietz DM, Park J, Clark SD. Intra-ventral tegmental area microinjections of urotensin II modulate the effects of cocaine. Behav Brain Res. 2015 Feb 1;278:271-9. doi: 10.1016/j.bbr.2014.09.036. Epub 2014 Oct 1. PMID: 25264578; PMCID: PMC4382453.
6: Park SL, Lee BK, Kim YA, Lee BH, Jung YS. Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Induced by Urotensin II in Human Vascular Endothelial Cells. Biomol Ther (Seoul). 2013 Jul 30;21(4):277-83. doi: 10.4062/biomolther.2013.051. PMID: 24244812; PMCID: PMC3819900.
7: Adebiyi A. RGS2 regulates urotensin II-induced intracellular Ca2+ elevation and contraction in glomerular mesangial cells. J Cell Physiol. 2014 Apr;229(4):502-11. doi: 10.1002/jcp.24470. PMID: 24105430.
8: Watson AM, Olukman M, Koulis C, Tu Y, Samijono D, Yuen D, Lee C, Behm DJ, Cooper ME, Jandeleit-Dahm KA, Calkin AC, Allen TJ. Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia. 2013 May;56(5):1155-65. doi: 10.1007/s00125-013-2837-9. Epub 2013 Jan 24. PMID: 23344731.
9: You Z, Genest J Jr, Barrette PO, Hafiane A, Behm DJ, D'Orleans-Juste P, Schwertani AG. Genetic and pharmacological manipulation of urotensin II ameliorate the metabolic and atherosclerosis sequalae in mice. Arterioscler Thromb Vasc Biol. 2012 Aug;32(8):1809-16. doi: 10.1161/ATVBAHA.112.252973. Epub 2012 Jun 21. PMID: 22723440.
10: Oh KS, Lee S, Lee BH. Development of filtration-based time-resolved fluorescence assay for the high-throughput screening of urotensin II receptor antagonist. Assay Drug Dev Technol. 2011 Oct;9(5):514-21. doi: 10.1089/adt.2010.0353. Epub 2011 May 11. PMID: 21561377.
11: Kompa AR, Wang BH, Phrommintikul A, Ho PY, Kelly DJ, Behm DJ, Douglas SA, Krum H. Chronic urotensin II receptor antagonist treatment does not alter hypertrophy or fibrosis in a rat model of pressure-overload hypertrophy. Peptides. 2010 Aug;31(8):1523-30. doi: 10.1016/j.peptides.2010.04.026. Epub 2010 May 7. PMID: 20452383.
12: Behm DJ, McAtee JJ, Dodson JW, Neeb MJ, Fries HE, Evans CA, Hernandez RR, Hoffman KD, Harrison SM, Lai JM, Wu C, Aiyar NV, Ohlstein EH, Douglas SA. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30. PMID: 18587423; PMCID: PMC2567886.
13: Douglas SA, Behm DJ, Aiyar NV, Naselsky D, Disa J, Brooks DP, Ohlstein EH, Gleason JG, Sarau HM, Foley JJ, Buckley PT, Schmidt DB, Wixted WE, Widdowson K, Riley G, Jin J, Gallagher TF, Schmidt SJ, Ridgers L, Christmann LT, Keenan RM, Knight SD, Dhanak D. Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br J Pharmacol. 2005 Jul;145(5):620-35. doi: 10.1038/sj.bjp.0706229. PMID: 15852036; PMCID: PMC1576177.
