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Chemical Structure| 211096-49-0 Chemical Structure| 211096-49-0

Structure of SB-265610
CAS No.: 211096-49-0

Chemical Structure| 211096-49-0

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SB-265610 is a potent CXCR2 antagonist that inhibits CINC-1-mediated but not C5a-mediated Ca2+ mobilization (IC50 values are 3.4 and 6800 nM respectively). It inhibits CINC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo.

Synonyms: SB-265610

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Product Details of SB-265610

CAS No. :211096-49-0
Formula : C14H9BrN6O
M.W : 357.16
SMILES Code : O=C(NC1=C2NN=NC2=C(C#N)C=C1)NC3=CC=CC=C3Br
Synonyms :
SB-265610
MDL No. :MFCD09971124

Safety of SB-265610

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SB-265610

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CHO cells expressing human CXCR2 receptor 1-30 nM 2 hours To investigate the effect of SB265610 on [125I]-IL-8 binding, results showed that SB265610 reduced the maximal binding of [125I]-IL-8 without affecting the Kd. Br J Pharmacol. 2009 Sep;158(1):328-38
Human neutrophils 10-1000 nM 30 minutes To investigate the effect of SB265610 on GROα-stimulated chemotaxis, results showed that SB265610 caused a rightward shift of the concentration-response curves to GROα, but no effect on the maximal response. Br J Pharmacol. 2009 Sep;158(1):328-38

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Bronchopulmonary dysplasia (BPD) model Intraperitoneal injection 1 mg/kg Administered on P1, P3, and P5 CXCR2 antagonist significantly attenuated the LPS-induced increase in neutrophil counts in BALF and PB and restored alveolarization, as indicated by decreased mean cord length and increased alveolar surface area. Clin Exp Pediatr. 2021 Jan;64(1):37-43
C57 black mice CXCR2 wild type mice Oral 100 mg/kg/day Once daily for 5 days To evaluate the effect of CXCR2 antagonist on wound healing. Results showed that SB-265610 markedly delayed the wound healing process and reduced MPO activity at the wound site. Wound Repair Regen. 2003 May-Jun;11(3):213-9

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

14.00mL

2.80mL

1.40mL

28.00mL

5.60mL

2.80mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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