貨號	規格	價格	上海	北京	武漢	南京
S84705-5mg	99.8%	￥400.00 S84705-5mg ￥400.00 現貨	5 5	-	-	-
S84705-10mg	99.8%	￥790.00 S84705-10mg ￥790.00 現貨	9 9	-	-	-
S84705-25mg	99.8%	￥1300.00 S84705-25mg ￥1300.00 現貨	5 5	-	-	-
S84705-100mg	99.8%	￥3500.00 S84705-100mg ￥3500.00 現貨	7 7	-	-	-

產品介紹

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

產品描述：

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

靶點：

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

體內研究：

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.)

參考文獻：

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)

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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