| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SB-657510 primarily targets the urotensin-II (UII) receptor (UT receptor, also known as GPR14), a G protein-coupled receptor involved in cardiovascular regulation and inflammation. It acts as a selective, non-peptide antagonist with Ki values of 61 nM (human), 17 nM (monkey), 30 nM (cat), 65 nM (rat), and 56 nM (mouse). By blocking UT receptor, SB-657510 inhibits UII-induced inflammatory mediators in vascular endothelial cells.
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| ln Vitro |
The UII-induced increase in adhesion between EA.hy926 and U937 cells is greatly inhibited by SB-657510. In endothelial cells, SB-657510 (1 μM; 0.5-8 hours) inhibits the production of tissue factors produced by UII [1]. With an IC50 of 180 nM, SB-706375 (1-10000 nM) suppresses the [Ca2+]i mobilization mediated by 10 nM hU-II[2].
In vitro, SB-657510 functions as a selective UT receptor antagonist. It inhibits UII-induced inflammatory mediators, such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells. The compound inhibits UII-mediated cell adhesion and tissue factor expression. Its activity is measured in receptor binding and functional assays using cells expressing UT receptors. Ki values are determined from radioligand binding assays. |
| ln Vivo |
SB-657510 reduces the advancement of high-fat diet-induced atherosclerosis and diabetes-related atherosclerosis [1]. Phosphorylated ERK levels were dramatically reduced in the aorta of diabetic mice (male Apoe KO animals) treated with SB-657510 (30 mg/kg/day) [3].
In vivo, SB-657510 slows development of diabetes-associated atherosclerosis in mouse models of diabetes. It reduces ERK phosphorylation in diabetic mouse aortas. The compound has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models. By blocking UII-induced inflammatory mediators, SB-657510 exerts anti-inflammatory effects. Its in vivo efficacy has been demonstrated in models of diabetes and atherosclerosis. |
| Enzyme Assay |
Cell-free assays for SB-657510 involve evaluating its binding affinity to UT receptors. Radioligand binding assays are performed using membrane preparations from cells expressing human, monkey, cat, rat, or mouse UT receptors. SB-657510 is incubated with membranes and a radiolabeled UT receptor ligand. Competition binding experiments determine Ki values for each species. Selectivity is assessed by testing against other receptors. Chemical purity and identity are confirmed by HPLC and NMR analysis.
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| Cell Assay |
Western Blot analysis [1]
Cell Types: EA.hy926 cells (UII induced) Tested Concentrations: 1 μM Incubation Duration: 0.5, 1, 2, 4, 8 hrs (hours) Experimental Results: Dramatically diminished UII-induced tissue factor protein expression. In vitro cellular assays for SB-657510 typically involve treating human vascular endothelial cells with various concentrations of the compound. Cells are stimulated with UII to induce inflammatory responses. Adhesion molecule, cytokine, and tissue factor expression is measured by qPCR, ELISA, or western blotting. Cell adhesion assays are performed to assess functional effects. The compound's ability to inhibit UII-induced inflammatory mediators is assessed. Dose-response curves are generated to determine potency. |
| Animal Protocol |
In vivo animal studies for SB-657510 are conducted in mouse models of diabetes and atherosclerosis. The compound is administered via various routes including oral gavage or intraperitoneal injection. Atherosclerotic plaque development is assessed by histological analysis. ERK phosphorylation in aortas is measured by western blotting. Inflammatory markers in serum and tissues are measured using ELISA. Efficacy is evaluated by comparing disease progression between treatment and control groups.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SB-657510 include a molecular weight of 485.36 g/mol and molecular formula C19H22BrClN2O5S. As a small molecule antagonist, it is expected to have moderate oral bioavailability and tissue penetration. The compound is typically stored at appropriate conditions as a research reagent. Detailed ADME parameters such as half-life, Cmax, and AUC are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of SB-657510 has been characterized in preclinical studies. As a UT receptor antagonist, potential toxicities may include effects on cardiovascular function. Standard toxicology studies would include acute and sub-chronic toxicity assessments in rodent models. The compound is intended for research use only and not for therapeutic applications in humans. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
SB-657510 is a potent and selective urotensin-II (UT) receptor antagonist with Ki values of 61, 17, 30, 65, and 56 nM at human, monkey, cat, rat, and mouse receptors. It exerts anti-inflammatory activity by blocking UII-induced upregulation of adhesion molecules and cytokines in vascular endothelial cells. SB-657510 slows diabetes-associated atherosclerosis in mouse models. It is a research tool for studying urotensin-II signaling and cardiovascular disease.
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| Molecular Formula |
C₁₉H₂₂BRCLN₂O₅S
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| Molecular Weight |
505.81
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| Exact Mass |
504.012
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| CAS # |
474960-44-6
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| PubChem CID |
11272107
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| Appearance |
White to off-white solid powder
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| LogP |
5.095
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
637
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CC[C@H](C1)OC2=C(C=CC(=C2)NS(=O)(=O)C3=C(C=C(C(=C3)OC)OC)Br)Cl
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| InChi Key |
KQCZCINJGIRLCD-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C19H22BrClN2O5S/c1-23-7-6-13(11-23)28-16-8-12(4-5-15(16)21)22-29(24,25)19-10-18(27-3)17(26-2)9-14(19)20/h4-5,8-10,13,22H,6-7,11H2,1-3H3/t13-/m1/s1
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| Chemical Name |
2-bromo-N-[4-chloro-3-[(3R)-1-methylpyrrolidin-3-yl]oxyphenyl]-4,5-dimethoxybenzenesulfonamide
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| Synonyms |
SB657510; SB-657510
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~197.70 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9770 mL | 9.8851 mL | 19.7703 mL | |
| 5 mM | 0.3954 mL | 1.9770 mL | 3.9541 mL | |
| 10 mM | 0.1977 mL | 0.9885 mL | 1.9770 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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