Reparixin
Based on 63 publication(s) in Google Scholar
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 266359-83-5
- Formula: C14H21NO3S
- Molecular Weight:283.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Reparixin
More- Science. 2026 Mar 26;391(6792):eadz9353. [Abstract]
- Cancer Cell. 2023 Apr 10;41(4):693-710.e8. [Abstract]
- Ann Rheum Dis. 2016 Apr;75(4):721-9. [Abstract]
- Ann Rheum Dis. 2016 Apr;75(4):730-8. [Abstract]
- Nat Commun. 2017 May 26;8:15584. [Abstract]
- Adv Sci (Weinh). 2025 Jan 30:e2406218. [Abstract]
- Adv Sci (Weinh). 2024 Sep 13:e2403430. [Abstract]
- Sci Adv. 2019 May 8;5(5):eaav7384. [Abstract]
- J Biomed Sci. 2025 Jan 6;32(1):5. [Abstract]
- Mol Ther. 2022 Nov 2;30(11):3430-3449. [Abstract]
- J Allergy Clin Immunol. 2018 Jun;141(6):2286-2289.e5. [Abstract]
- EBioMedicine. 2019 May:43:487-500. [Abstract]
- Cancer Lett. 2026 May 1:645:218395. [Abstract]
- Mol Biomed. 2025 Jun 10;6(1):40. [Abstract]
- Cell Death Dis. 2017 Jul 13;8(7):e2932. [Abstract]
- Cell Commun Signal. 2023 Mar 13;21(1):59. [Abstract]
- Dev Cell. 2026 Jan 12:S1534-5807(25)00768-3. [Abstract]
- BMC Med. 2022 Feb 8;20(1):55. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2024 May 7:S2352-345X(24)00105-X. [Abstract]
- Int Endod J. 2026 Jun 24. [Abstract]
- Oncogenesis. 2016 Jun 13;5(6):e234. [Abstract]
- Brain Pathol. 2024 Jun 30:e13283. [Abstract]
- Cell Biosci. 2019 Jan 3:9:4. [Abstract]
- Cancer Cell Int. 2021 Jul 3;21(1):337. [Abstract]
- J Mol Cell Biol. 2023 Aug 3;15(4):mjad025. [Abstract]
- Front Immunol. 2022 Oct 17:13:1007341. [Abstract]
- Front Immunol. 2021 May 7;12:667177. [Abstract]
- Front Immunol. 2018 Sep 12:9:2058. [Abstract]
- Neurobiol Dis. 2021 Dec:160:105538. [Abstract]
- Cells. 2026 Feb 3;15(3):289. [Abstract]
- Cells. 2022 Aug 4;11(15):2402. [Abstract]
- Cells. 2022 Jun 21;11(13):1986. [Abstract]
- Cancers (Basel). 2023 Sep 4;15(17):4422. [Abstract]
- J Cell Mol Med. 2020 Nov;24(21):12608-12618. [Abstract]
- J Cell Mol Med. 2020 Jan;24(2):1588-1598. [Abstract]
- J Mol Med (Berl). 2019 Jan;97(1):25-35. [Abstract]
- Biochim Biophys Acta. 2017 Jan;1863(1):220-230. [Abstract]
- Xenotransplantation. 2018 Mar;25(2):e12385. [Abstract]
- Sci Rep. 2017 Nov 6;7(1):14510. [Abstract]
- Brain Res Bull. 2025 Oct 22:232:111594. [Abstract]
- Stem Cells. 2015 Dec;33(12):3558-68. [Abstract]
- J Immunol. 2018 Jul 15;201(2):814-820. [Abstract]
- J Gastroenterol Hepatol. 2018 Feb;33(2):431-442. [Abstract]
- Mol Immunol. 2018 Sep:101:440-449. [Abstract]
- FACETS. 2020 Jul.
- Gene. 2018 Nov 30:677:149-162. [Abstract]
- Biomed Res Int. 2020 Aug 5;2020:4670604. [Abstract]
- Vet Immunol Immunopathol. 2016 Dec:182:52-58. [Abstract]
- bioRxiv. 2025 Sep 3:2025.09.02.672566. [Abstract]
- bioRxiv. 2025 Mar 19:2025.03.19.644113. [Abstract]
- Patent. US20240295544A1.
- bioRxiv. 2024 Jun 6:2024.01.30.577927. [Abstract]
- Patent. US20220251222A1.
- Karolinska Institutet. 2022 Feb.
- Int J Biol Sci. 2022 Jan 16;18(4):1363-1380. [Abstract]
- Research Square Preprint. 2021 Mar.
- bioRxiv. 2020 Sep 12:2020.08.25.265561. [Abstract]
- University of Michigan. 2018 Oct.
- Oncotarget. 2018 Aug 24;9(66):32556-32569. [Abstract]
- Oncotarget. 2017 Jul 21;8(36):60210-60222. [Abstract]
- Patent. US20170181987A1.
- Patent. US20170105971A1.
- Johns Hopkins University. 2016 Dec.
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IF
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Cell Proliferation/Viability Assay
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IF
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Cell Proliferation/Viability Assay
Biological Activity
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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) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| L1.2 | IC50 |
0.0056 μM
Compound: raparixin
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Inhibition of CXCL8-induced cell migration in L1.2 cells expressing CXCR1 by chemotaxis assay
Inhibition of CXCL8-induced cell migration in L1.2 cells expressing CXCR1 by chemotaxis assay
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[PMID: 17665889] |
| L1.2 | IC50 |
0.08 μM
Compound: raparixin
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Inhibition of CXCL8-induced cell migration in L1.2 cells expressing Ile43Val CXCR1 mutant by chemotaxis assay
Inhibition of CXCL8-induced cell migration in L1.2 cells expressing Ile43Val CXCR1 mutant by chemotaxis assay
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[PMID: 17665889] |
Reparixin is a potent functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively)[1]. Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 266359-83-5
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Appearance Solid
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Molecular Weight 283.39
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Formula C14H21NO3S
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Color White to off-white
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SMILES
CS(=O)(NC([C@@H](C1=CC=C(CC(C)C)C=C1)C)=O)=O
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Synonyms
Repertaxin; DF 1681Y
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (63)
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Journal Impact Factor
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Most Recent
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Science
2026 Mar 26;391(6792):eadz9353. PMID: 41538410 -
Cancer Cell
2023 Apr 10;41(4):693-710.e8. PMID: 36963400 -
Ann Rheum Dis
Identification of a novel chemokine-dependent molecular mechanism underlying rheumatoid arthritis-associated autoantibody-mediated bone loss. [Abstract]2016 Apr;75(4):721-9. PMID: 26612338 -
Ann Rheum Dis
Autoantibodies to citrullinated proteins induce joint pain independent of inflammation via a chemokine-dependent mechanism. [Abstract]2016 Apr;75(4):730-8. PMID: 26613766 -
Nat Commun
Synergistic IL-6 and IL-8 paracrine signalling pathway infers a strategy to inhibit tumour cell migration. [Abstract]2017 May 26;8:15584. PMID: 28548090 -
Adv Sci (Weinh)
Single-Cell Landscape of Bronchoalveolar Lavage Fluid Identifies Specific Neutrophils during Septic Immunosuppression. [Abstract]2025 Jan 30:e2406218. PMID: 39887584 -
Adv Sci (Weinh)
SKAP1 Expression in Cancer Cells Enhances Colon Tumor Growth and Impairs Cytotoxic Immunity by Promoting Neutrophil Extracellular Trap Formation via the NFATc1/CXCL8 Axis. [Abstract]2024 Sep 13:e2403430. PMID: 39269257 -
Sci Adv
Differentiated fibrocytes assume a functional mesenchymal phenotype with regenerative potential. [Abstract]2019 May 8;5(5):eaav7384. PMID: 31086819 -
J Biomed Sci
Fusobacterium nucleatum promotes colorectal cancer liver metastasis via miR-5692a/IL-8 axis by inducing epithelial-mesenchymal transition. [Abstract]2025 Jan 6;32(1):5. PMID: 39757156 -
Mol Ther
Engineered bispecific antibodies targeting the interleukin-6 and -8 receptors potently inhibit cancer cell migration and tumor metastasis. [Abstract]2022 Nov 2;30(11):3430-3449. PMID: 35841152 -
J Allergy Clin Immunol
Human TH17 cell development requires processing of dendritic cell-derived CXCL8 by neutrophil elastase. [Abstract]2018 Jun;141(6):2286-2289.e5. PMID: 29391256 -
EBioMedicine
Interleukin-8 as a therapeutic target for chronic low back pain: Upregulation in human cerebrospinal fluid and pre-clinical validation with chronic reparixin in the SPARC-null mouse model. [Abstract]2019 May:43:487-500. PMID: 31047862 -
Cancer Lett
DysUFMylation reprograms immunosuppressive neutrophils to potentiate anti-PD-1 therapy in hepatocellular carcinoma. [Abstract]2026 May 1:645:218395. PMID: 41780840 -
Mol Biomed
C-X-C motif chemokine ligand 1 derived from oral squamous cell carcinoma promotes cancer-associated fibroblast differentiation and tumor growth. [Abstract]2025 Jun 10;6(1):40. PMID: 40490643 -
Cell Death Dis
An autocrine inflammatory forward-feedback loop after chemotherapy withdrawal facilitates the repopulation of drug-resistant breast cancer cells. [Abstract]2017 Jul 13;8(7):e2932. PMID: 28703802 -
Cell Commun Signal
Paracrine secretion of IL8 by breast cancer stem cells promotes therapeutic resistance and metastasis of the bulk tumor cells. [Abstract]2023 Mar 13;21(1):59. PMID: 36915147 -
Dev Cell
MITA/STING-driven CD38 induction in Siglec-Flow macrophages promotes regulatory T cell survival and non-small cell lung cancer progression. [Abstract]2026 Jan 12:S1534-5807(25)00768-3. PMID: 41529690 -
BMC Med
Upregulation of NOD1 and NOD2 contribute to cancer progression through the positive regulation of tumorigenicity and metastasis in human squamous cervical cancer. [Abstract]2022 Feb 8;20(1):55. PMID: 35130902 -
Cell Mol Gastroenterol Hepatol
Concomitant NAFLD Facilitates Liver Metastases and PD-1-Refractory by Recruiting MDSCs via CXCL5/CXCR2 in Colorectal Cancer. [Abstract]2024 May 7:S2352-345X(24)00105-X. PMID: 38724007 -
Int Endod J
The Interplay of M1 Macrophages and Dental Pulp Stem Cells Promotes Angiogenesis Through IL-8-Dependent VEGF Regulation: An In Vitro Study. [Abstract]2026 Jun 24. PMID: 42339579 -
Oncogenesis
Loss of OLFM4 promotes tumor migration through inducing interleukin-8 expression and predicts lymph node metastasis in early gastric cancer. [Abstract]2016 Jun 13;5(6):e234. PMID: 27294866
Reparixin purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2016 Jun 13;5(6):e234. [Abstract]
The effects of Reparixin (100 nM) on the migration of OLFM4-depleted gastric cancer cells are detected by transwell assay.
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Brain Pathol
Intracerebellar administration of the chemokine Cxcl3 reduces the volume of medulloblastoma lesions at an advanced stage by promoting the migration and differentiation of preneoplastic precursor cells. [Abstract]2024 Jun 30:e13283. PMID: 38946128 -
Cell Biosci
1-Palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) attenuates gemcitabine-induced neutrophil extravasation. [Abstract]2019 Jan 3:9:4. PMID: 30622698 -
Cancer Cell Int
SHP2 inhibition enhances the anticancer effect of Osimertinib in EGFR T790M mutant lung adenocarcinoma by blocking CXCL8 loop mediated stemness. [Abstract]2021 Jul 3;21(1):337. PMID: 34217295 -
J Mol Cell Biol
CSF2 upregulates CXCL3 expression in adipocytes to promote metastasis of breast cancer via the FAK signaling pathway. [Abstract]2023 Aug 3;15(4):mjad025. PMID: 37073091 -
Front Immunol
CXCR1 and its downstream NF-κB inflammation signaling pathway as a key target of Guanxinning injection for myocardial ischemia/reperfusion injury. [Abstract]2022 Oct 17:13:1007341. PMID: 36325326
Reparixin purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 Oct 17:13:1007341. [Abstract]
In HL-1 cells, when DSS and Reparixin (100nM) are applied in combination, the high expression levels of NF-κB, COX-2, ICAM-1 and VCAM-1 induced by OGD/R are further inhibited compared with that of DSS alone.
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Front Immunol
CXCL8 Associated Dendritic Cell Activation Marker Expression and Recruitment as Indicators of Favorable Outcomes in Colorectal Cancer. [Abstract]2021 May 7;12:667177. PMID: 34025668 -
Front Immunol
Amphibian ( Xenopus laevis) Interleukin-8 (CXCL8): A Perspective on the Evolutionary Divergence of Granulocyte Chemotaxis. [Abstract]2018 Sep 12:9:2058. PMID: 30258441 -
Neurobiol Dis
CXCR2 increases in ALS cortical neurons and its inhibition prevents motor neuron degeneration in vitro and improves neuromuscular function in SOD1G93A mice. [Abstract]2021 Dec:160:105538. PMID: 34743985 -
Cells
2026 Feb 3;15(3):289. PMID: 41677651 -
Cells
The AGEs/RAGE Transduction Signaling Prompts IL-8/CXCR1/2-Mediated Interaction between Cancer-Associated Fibroblasts (CAFs) and Breast Cancer Cells. [Abstract]2022 Aug 4;11(15):2402. PMID: 35954247 -
Cells
2022 Jun 21;11(13):1986. PMID: 35805071 -
Cancers (Basel)
Novel Function of Cancer Stem Cell Marker ALDH1A3 in Glioblastoma: Pro-Angiogenesis through Paracrine PAI-1 and IL-8. [Abstract]2023 Sep 4;15(17):4422. PMID: 37686698 -
J Cell Mol Med
Neuropilin-1 is up-regulated by cancer-associated fibroblast-secreted IL-8 and associated with cell proliferation of gallbladder cancer. [Abstract]2020 Nov;24(21):12608-12618. PMID: 32951327 -
J Cell Mol Med
IL-8 promotes cell migration through regulating EMT by activating the Wnt/β-catenin pathway in ovarian cancer. [Abstract]2020 Jan;24(2):1588-1598. PMID: 31793192 -
J Mol Med (Berl)
Propionibacterium acnes induces discogenic low back pain via stimulating nucleus pulposus cells to secrete pro-algesic factor of IL-8/CINC-1 through TLR2-NF-κB p65 pathway. [Abstract]2019 Jan;97(1):25-35. PMID: 30397790 -
Biochim Biophys Acta
The matrikine N-acetylated proline-glycine-proline induces premature senescence of nucleus pulposus cells via CXCR1-dependent ROS accumulation and DNA damage and reinforces the destructive effect of these cells on homeostasis of intervertebral discs. [Abstract]2017 Jan;1863(1):220-230. PMID: 27769935 -
Xenotransplantation
Interleukin-8 mediates neutrophil-endothelial interactions in pig-to-human xenogeneic models. [Abstract]2018 Mar;25(2):e12385. PMID: 29427404 -
Sci Rep
Protein profiling identified key chemokines that regulate the maintenance of human pluripotent stem cells. [Abstract]2017 Nov 6;7(1):14510. PMID: 29109449 -
Brain Res Bull
Multi-omics analysis reveals the protective role of transcriptional enhancer factor and the pathogenic mechanism of monocytes in Parkinson's disease. [Abstract]2025 Oct 22:232:111594. PMID: 41135742 -
Stem Cells
Collagen-Derived N-Acetylated Proline-Glycine-Proline in Intervertebral Discs Modulates CXCR1/2 Expression and Activation in Cartilage Endplate Stem Cells to Induce Migration and Differentiation Toward a Pro-Inflammatory Phenotype. [Abstract]2015 Dec;33(12):3558-68. PMID: 26302999 -
J Immunol
2018 Jul 15;201(2):814-820. PMID: 29802127 -
J Gastroenterol Hepatol
High expression of tumor necrosis factor receptor-associated factor 2 promotes tumor metastasis and is associated with unfavorable prognosis in gastric cancer. [Abstract]2018 Feb;33(2):431-442. PMID: 28482378
Reparixin purchased from MedChemExpress. Usage Cited in: J Gastroenterol Hepatol. 2018 Feb;33(2):431-442. [Abstract]
The effects of TRAF2 overexpression with or without Reparixin (100 nM), or BAY 11-7082 (30 μM) on the migration and invasion of AGS cell are examined by transwell assay.
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Mol Immunol
Interleukin 8 (CXCL8)-CXC chemokine receptor 2 (CXCR2) axis contributes to MiR-4437-associated recruitment of granulocytes and natural killer cells in ischemic stroke. [Abstract]2018 Sep:101:440-449. PMID: 30096583 -
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Gene
Conserved structure and function of chemokine CXCL8 between Chinese tree shrews and humans. [Abstract]2018 Nov 30:677:149-162. PMID: 30012425 -
Biomed Res Int
Icariin Ameliorates Lower Back Pain in Rats via Suppressing the Secretion of Cytokine-Induced Neutrophil Chemoatractant-1. [Abstract]2020 Aug 5;2020:4670604. PMID: 32802846 -
Vet Immunol Immunopathol
CC chemokine ligand 2 and CXC chemokine ligand 8 as neutrophil chemoattractant factors in canine idiopathic polyarthritis. [Abstract]2016 Dec:182:52-58. PMID: 27863550 -
bioRxiv
2025 Sep 3:2025.09.02.672566. PMID: 40950232 -
bioRxiv
Mast cells interact directly with colorectal cancer cells to promote epithelial-to-mesenchymal transition. [Abstract]2025 Mar 19:2025.03.19.644113. PMID: 40166179 -
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bioRxiv
2024 Jun 6:2024.01.30.577927. PMID: 38352492 -
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Int J Biol Sci
Cancer-associated adipocytes promote the invasion and metastasis in breast cancer through LIF/CXCLs positive feedback loop. [Abstract]2022 Jan 16;18(4):1363-1380. PMID: 35280694 -
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bioRxiv
SARS-CoV-2 infection of human iPSC-derived cardiac cells predicts novel cytopathic features in hearts of COVID-19 patients. [Abstract]2020 Sep 12:2020.08.25.265561. PMID: 32935097 -
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Oncotarget
2018 Aug 24;9(66):32556-32569. PMID: 30220965 -
Oncotarget
Crosstalk between stromal components and tumor cells of TNBC via secreted factors enhances tumor growth and metastasis. [Abstract]2017 Jul 21;8(36):60210-60222. PMID: 28947965
Reparixin purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 21;8(36):60210-60222. [Abstract]
Migration assay of MDA-MB-231 cells treated 0.1 uM of Reparixin in CM from fibroblasts or macrophages with TCM of MDA-MB-231 cells using the Oris Cell migration kit.
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (352.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37°C for 15 min in the presence of vehicle or of Reparixin (1 nM-1μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber. Different agonists are seeded in the lower compartment of the chamber at the following concentrations: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, 30 nM C5a. The chemotactic chamber is incubated at 37°C in air with 5% CO2 for 45 min (human PMNs) or 2 h (monocytes). At the end of incubation, the filter is removed, fixed, and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding. L1.2 migration is evaluated using 5 μm pore size Transwell filters[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[3]
The Reparixin-treated group contained 5 SHR (SHR-R), where equal numbers of normal saline-treated SHR (SHR-N) and WKY (WKY-N) served as controls. Eighteen-week-old SHR received a subcutaneous injection of Reparixin (5 mg/kg) once per day for 3 weeks. Reparixin effects on blood flow, blood pressure and body weight are measured before treatment and then weekly until 1 week after the final injection. The effect of Reparixin on the expression of hypertension-related mediators in thoracic aortas, as well as nitric oxide (NO) plasma levels, is examined 1 week after the final injection.
Mice[4]
C57BL/6J mice (8-10 weeks old/20-25 g) are used. The subcutaneous administration of Reparixin (30 mg/kg) is performed 60 minutes before cerebral ischemia induction. The animals are divided into the following three experimental groups: Sham (i.e., the group in which the arteries are visualized, but there is no occlusion of the middle cerebral artery), Vehicle (i.e., the group pre-treated with the vehicle, phosphate buffer solution, 60 minutes before MCAo) and Reparixin (i.e., the group pre-treated with the drug 60 minutes before MCAo). To evaluate neurological signs secondary to MCAo, the animals are assessed with the SHIRPA battery 24 h after reperfusion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[7]. Crespo J, et al. Human Naive T Cells Express Functional CXCL8 and Promote Tumorigenesis. J Immunol. 2018 Jul 15;201(2):814-820. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5287 mL | 17.6435 mL | 35.2871 mL | 88.2176 mL |
| 5 mM | 0.7057 mL | 3.5287 mL | 7.0574 mL | 17.6435 mL | |
| 10 mM | 0.3529 mL | 1.7644 mL | 3.5287 mL | 8.8218 mL | |
| 15 mM | 0.2352 mL | 1.1762 mL | 2.3525 mL | 5.8812 mL | |
| 20 mM | 0.1764 mL | 0.8822 mL | 1.7644 mL | 4.4109 mL | |
| 25 mM | 0.1411 mL | 0.7057 mL | 1.4115 mL | 3.5287 mL | |
| 30 mM | 0.1176 mL | 0.5881 mL | 1.1762 mL | 2.9406 mL | |
| 40 mM | 0.0882 mL | 0.4411 mL | 0.8822 mL | 2.2054 mL | |
| 50 mM | 0.0706 mL | 0.3529 mL | 0.7057 mL | 1.7644 mL | |
| 60 mM | 0.0588 mL | 0.2941 mL | 0.5881 mL | 1.4703 mL | |
| 80 mM | 0.0441 mL | 0.2205 mL | 0.4411 mL | 1.1027 mL | |
| 100 mM | 0.0353 mL | 0.1764 mL | 0.3529 mL | 0.8822 mL |