产品说明书

Reparixin

Print
Chemical Structure| 266359-83-5 同义名 : Repertaxin;DF 1681Y
CAS号 : 266359-83-5
货号 : A730164
分子式 : C14H21NO3S
纯度 : 99%+
分子量 : 283.386
MDL号 : MFCD18633292
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(370.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CXCR1
描述 CXC chemokines CXCL8 and CXCL1 play essential roles in the activation and recruitment of neutrophils. CXCR1 and CXCR2 are two membrane receptors that bind to CXCL8 with high affinity. Reparixin is a small-molecule, allosteric CXCR1 inhibitor. Reparixin at 0.1 μM led to an 80% inhibition on CXCL8 (10 nM)-induced wild-type CXCR1/L1.2 transfectants migration. The efficacy of reparixin in cells expressing CXCR1 WT and Ile43Val CXCR1 mutant were significantly different (IC50 values of 5.6 and 80 nM, respectively)[3]. In C57BL/6 mice, subcutaneous administration with reparixin (30 mg/kg) reduced neutrophil activity in the brain after middle cerebral artery occlusion/reperfusion. Reparixin treatment also decreased the levels of interleukin-1β in the brain compared to the vehicle-treated group[4].
作用机制 Reparixin is a non-competitive allosteric CXCR1 inhibitor that binds to the transmembrane region of CXCR1, thereby effectively blocking agonist-induced receptor signaling in the intracellular compartment. However, reparixin does not directly affect the expressions of receptors or the CXCL8 binding affinity.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.64mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL
参考文献

[1]Bertini R, Barcelos LS, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2 non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54.

[2]Moriconi A, Cesta MC, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002.

[3]Moriconi A, Cesta MC, Cervellera MN, Aramini A, Coniglio S, Colagioia S, Beccari AR, Bizzarri C, Cavicchia MR, Locati M, Galliera E, Di Benedetto P, Vigilante P, Bertini R, Allegretti M. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002. doi: 10.1021/jm061469t. Epub 2007 Aug 1. PMID: 17665889.

[4]Sousa LF, Coelho FM, Rodrigues DH, Campos AC, Barcelos Lda S, Teixeira MM, Rachid MA, Teixeira AL. Blockade of CXCR1/2 chemokine receptors protects against brain damage in ischemic stroke in mice. Clinics (Sao Paulo). 2013;68(3):391-4. doi: 10.6061/clinics/2013(03)oa17. PMID: 23644861; PMCID: PMC3611745.