Reparixin
(Synonyms: 瑞帕利辛; Repertaxin; DF 1681Y) 目录号 : GC12849
An allosteric inhibitor of CXCR1 and CXCR2
Cas No.:266359-83-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
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Binding assays |
Isolated PMNs (107×mL) were resuspended in RPMI 1640 and incubated at 37℃ for 15 min in the presence of repertaxin (1 mM) or vehicle. After incubation cells were resuspended (2×107/mL) in binding medium (RPMI 1640 containing 10 mg/ml BSA, 20 mM HEPES, and 0.02% NaN3) in the presence of repertaxin or vehicle. Aliquots of 0.2 nM of [125I]CXCL8 and serial dilutions of unlabeled CXCL8 were added to 106 cells in 100 μL of binding medium and incubated at room temperature for 1 hr under gentle agitation. Unbound radioactivity was separated from cell-bound radioactivity by centrifugation through anoil gradient (80% silicon and 20% paraffin) on a microcentrifuge. Nonspecific binding was determined by a 200-fold molar excess of unlabeled CXCL8. Scatchard analysis was performed with the LIGAND program. |
| Cell experiment [1]: | |
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Cell lines |
Human polymorphonuclear cells (PMN) and monocytes and rodent peritoneal PMN. |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
45 min (human PMN), 1 h (rodent PMN), or 2 h (monocytes). |
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Applications |
Repertaxin inhibits human PMN migration induced by CXCL8 and CXCL1 with IC50 values of 1 nM and 400 nM respectively, which are mediated by CXCR1 and CXCR2, respectively. Repertaxin also inhibits rodent PMN chemotaxis induced by CXCL1 and CXCL2. |
| Animal experiment [1]: | |
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Animal models |
Rat model of liver postischaemia RI. |
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Dosage form |
3, 15, or 30 mg/kg; 15 min before reperfusion (i.v.) and 2 h after reperfusion (s.c.). |
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Applications |
Repertaxin (15 mg/kg) inhibits PMN recruitment into reperfused livers by 90% and significantly reducesliver damage. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Bertini R, Allegretti M, Bizzarri C, 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, 101(32): 11791-11796. | |
Reparixin is a non-competitive allosteric inhibitor of CXCR1/2.
CXCR is a 7-transmembrane G protein-coupled receptor. CXCR plays a critical role in the development of different models of ALI Following engagement of this receptor, the Gbg-complex dissociates from the Gai-subunit and can activate phosphoinositide-3 kinase, different subtypes of phospholipase C and P-Rex-1. The downstream effectors of these molecules initiate a broad range of functional responses, including arrest from rolling, cytoskeletal rearrangement, cell polarization, chemotaxis, degranulation and respiratory burst.
Reperixin, specifically blocks CXCR1/2-mediated mouse and human neutrophil migration in vitro without affecting other receptors. Reparixin reduces ligand binding to human CXCR1 and CXCR2, calcium influx and downstream signalling in response to human CXCL8 and neutrophil recruitment into the liver in a mouse model of ischaemia-reperfusion injury. Reparixin reduced neutrophil recruitment and liver damage by approximately 30% and 80% in a model of ischaemiareperfusion injury.[1,2]
Reparixin reduced oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells. The best beneficial outcome of reparixin treatment will require 7-day administration either by i.p. route (15 mg/kg) or subcutaneous infusion via osmotic pumps (10 mg/kg), reaching a steady blood level of 8 μg/ml. Methylprednisolone are used as a reference drug, and such treatment reduced cytokine production but failed to affect the rate of hind limb recovery. [1,2]
References:
[1] A Zarbock, M Allegretti and K Ley. Therapeutic inhibition of CXCR2 by Reparixin attenuates acute lung injury in mice. British Journal of Pharmacology (2008) 155, 357–364.
[2] Alfredo Gorio, Laura Madaschi, Giorgia Zadra et al. Reparixin, an Inhibitor of CXCR2 Function, Attenuates Inflammatory Responses and Promotes Recovery of Function after Traumatic Lesion to the Spinal Cord. doi:10.1124/jpet.107.123679.
| Cas No. | 266359-83-5 | SDF | |
| 别名 | 瑞帕利辛; Repertaxin; DF 1681Y | ||
| 化学名 | (2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide | ||
| Canonical SMILES | CC(C)CC1=CC=C(C=C1)C(C)C(=O)NS(=O)(=O)C | ||
| 分子式 | C14H21NO3S | 分子量 | 283.39 |
| 溶解度 | ≥ 14.15 mg/mL in DMSO, ≥ 47.3 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5287 mL | 17.6435 mL | 35.2871 mL |
| 5 mM | 0.7057 mL | 3.5287 mL | 7.0574 mL |
| 10 mM | 0.3529 mL | 1.7644 mL | 3.5287 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。