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SB-657510

Catalog No. T12848 CAS 474960-44-6

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

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SB-657510, CAS 474960-44-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 126.00
5 mg	In stock	$ 378.00
10 mg	In stock	$ 568.00
25 mg	In stock	$ 913.00
50 mg	In stock	$ 1,230.00
100 mg	In stock	$ 1,680.00
500 mg	In stock	$ 3,360.00
1 mL * 10 mM (in DMSO)	In stock	$ 423.00

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Purity: 98.03%

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Description	SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.
Targets&IC50	UTII receptor (human):61 nM, UTII receptor (monkey):17 nM, UTII receptor (cat):30 nM, UTII receptor (rat):65 nM, UTII receptor (mouse):56 nM
In vitro	The UII-induced increase in adhesion between U937 and EA.hy926 cells was blocked by SB-657510 dramatically. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells.[1] SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10 nM hU-II(IC50 of 180 nM).[2]
In vivo	The progression of high-fat diet-induced atherosclerosis and diabetes-associated atherosclerosis inhibited by SB-657510.[1] Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice).[3]

Molecular Weight	505.81
Formula	C19H22BrClN2O5S
CAS No.	474960-44-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.0 mg/mL (53.4 mM)

References and Literature

1. Park SL, et al. Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Inducedby Urotensin II in Human Vascular Endothelial Cells. Biomol Ther (Seoul). 2013;21(4):277-283. 2. Behm DJ, et al. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008;155(3):374-386. 3. Watson AM, et al. Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia. 2013;56(5):1155-1165.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets

hNTS1R agonist-1 Neurotensin(8-13) SR 142948 Substance P 1-9 aceate SORT-PGRN interaction inhibitor 1 (±)-AC 7954 hydrochloride NTRC-844 Neurotensin

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Keywords

SB-657510 474960-44-6 GPCR/G Protein Others Neurotensin Receptor SB 657510 SB657510 inhibitor inhibit

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