Reparixin

    
99%

Reparixin

源叶(MedMol)
S84705 一键复制产品信息
266359-83-5
C14H21NO3S
283.39
Reparixin (USAN/INN); RAPARIXIN; reparixin; DF 1681Y;
货号 规格 价格 上海 北京 武汉 南京 购买数量
S84705-5mg 99% ¥400.00 5 - - -
S84705-10mg 99% ¥790.00 9 - - -
S84705-25mg 99% ¥1300.00 8 - - -
S84705-100mg 99% ¥3500.00 7 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.

产品描述: Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
靶点: CXCR1wt:5.6 nM (IC50, in L1.2 cells);CXCR1Ile43Val:80 nM (IC50, in L1.2 cells);CXCR1:1 nM (IC50, in cells);CXCR2:∼100 nM (IC50, in cells);CXCR
体内研究: Reparixin is an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, has been shown to attenuate inflammatory responses in various injury models. Spontaneously hypertensive rats (SHR) are administered a subcutaneous injection of Reparixin (5 mg/kg) daily for 3 weeks. Reparixin effectively decreases systolic blood pressure and increased the blood flow. Reparixin reduces the levels of IL-1β in the brain after middle cerebral artery occlusion/reperfusion (MCAo) in mice. Bars represent levels of IL-1β (pg/100 mg) measured by ELISA in the brain tissues of mice subjected or not (SHAM) to MCAo and pretreated with vehicle or Reparixin (30 mg/kg, s.c.)
参考文献: 1. Moriconi A, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002. 2. Bertini R, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54. 3. Kim HY, et al. Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats. Biol Pharm Bull. 2011;34(1):120-7. 4. Sousa LF, et al. Blockade of CXCR1/2 chemokine receptors protects against brain damage in ischemic stroke in mice. Clinics (Sao Paulo). 2013;68(3):391-4. 5. Bertini R, et al. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6. 6. Krishnamurthy A, et al. Identification of a novel chemokine-dependent molecular mechanism underlying rheumatoid arthritis-associated autoantibody-mediated bone loss. Ann Rheum Dis. 2016 Apr;75(4):721-9. 7. Crespo J, et al. Human Naive T Cells Express Functional CXCL8 and Promote Tumorigenesis. J Immunol. 2018 Jul 15;201(2):814-820.
溶解性: DMSO  :  ≥  100  mg/mL  (352.87  mM)    H2O  :  <  0.1  mg/mL  (insoluble)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.529 ml 17.644 ml 35.287 ml
5 mM 0.706 ml 3.529 ml 7.057 ml
10 mM 0.353 ml 1.764 ml 3.529 ml
50 mM 0.071 ml 0.353 ml 0.706 ml
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参考文献

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