SB 265610 |
| Catalog No.GC13458 |
SB 265610은 선택적, 경쟁적, 비펩타이드성 및 알로스테릭 CXCR2 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 211096-49-0
Sample solution is provided at 25 µL, 10mM.
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SB 265610 is a potent CXCR2 antagonist that inhibits CINC-1-mediated Ca2+ mobilization with IC50 value of 3.4nM [1] [2].
CXCR2 is an integral membrane protein that specifically binds and responds to cytokines of the CXC chemokine family.
In isolated rat neutrophils stimulated with rat CINC-1, SB 265610 inhibited Ca2+ mobilization induced by CINC-1 with IC50 value of 3.4 nM in a dose-dependent way, while inhibited Ca2+ mobilization induced by C5a only with IC50 value of 6.8uM, which showed selectivity of the antagonist for CXCR2 [1]. In equilibrium saturation binding studies, SB265610 inhibited the binding of interleukin-8 without affecting the Kd. While, IL-8 couldn’t prevent binding of SB265610. SB265610 is an allosteric inverse agonist at the CXCR2 receptor [2].
In a hyperoxia rat model, newborn rats increased lung neutrophil content. Treatment with SB-265610 reduced hyperoxia-induced neutrophil accumulation in bronchoalveolar lavage and whole lung myeloperoxidase accumulation [1].
References:
[1]. Auten RL, Richardson RM, White JR, et al. Nonpeptide CXCR2 antagonist prevents neutrophil accumulation in hyperoxia-exposed newborn rats. J Pharmacol Exp Ther, 2001, 299(1): 90-95.
[2]. Bradley ME, Bond ME, Manini J, et al. SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor. Br J Pharmacol, 2009, 158(1): 328-338.
| Cas No. | 211096-49-0 | SDF | |
| Chemical Name | 1-(2-bromophenyl)-3-(7-cyano-2H-benzo[d][1,2,3]triazol-4-yl)urea | ||
| Canonical SMILES | BrC1=CC=CC=C1NC(NC2=CC=C(C#N)C3=NNN=C23)=O | ||
| Formula | C14H9BrN6O | M.Wt | 357.16 |
| Solubility | 3mg/mL in DMSO, 3mg/mL in DMF, 5mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7999 mL | 13.9993 mL | 27.9987 mL |
| 5 mM | 0.56 mL | 2.7999 mL | 5.5997 mL |
| 10 mM | 0.28 mL | 1.3999 mL | 2.7999 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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