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Reparixin

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

Product Specifications

CAS Number

[266359-83-5]

Product Name Alternative

Repertaxin; DF 1681Y

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CXCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/Reparixin.html

Purity

99.99

Solubility

DMSO : ≥ 100 mg/mL|H2O : < 0.1 mg/mL

Smiles

CS(=O)(NC([C@@H](C1=CC=C(CC(C)C)C=C1)C)=O)=O

Molecular Formula

C14H21NO3S

Molecular Weight

283.39

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

CXCR1; CXCR2

Citation 01

Adv Sci (Weinh) . 2024 Sep 13:e2403430.|Adv Sci (Weinh) . 2025 Jan 30:e2406218.|Ann Rheum Dis. 2016 Apr;75 (4) :730-8.|Biochim Biophys Acta. 2017 Jan;1863 (1) :220-230.|bioRxiv. 2024 Jun 6:2024.01.30.577927.|bioRxiv. 2025 Mar 19:2025.03.19.644113.|bioRxiv. 2025 Sep 3:2025.09.02.672566.|BMC Med. 2022 Feb 8;20 (1) :55.|Brain Pathol. 2024 Jun 30:e13283.|Brain Res Bull. 2025 Oct 22:232:111594.|Cancer Cell Int. 2021 Jul 3;21 (1) :337.|Cancer Cell. 2023 Apr 10;41 (4) :693-710.e8.|Cancers (Basel) . 2023 Sep 4;15 (17) :4422.|Cell Biosci. 2019 Jan 3:9:4.|Cell Commun Signal. 2023 Mar 13;21 (1) :59.|Cell Death Dis. 2017 Jul 13;8 (7) :e2932.|Cell Mol Gastroenterol Hepatol. 2024 May 7:S2352-345X (24) 00105-X.|Cells. 2022 Aug 4;11 (15) :2402.|Cells. 2022 Jun 21;11 (13) :1986.|EBioMedicine. 2019 May:43:487-500.|FACETS. 2020 Jul.|Front Immunol. 2018 Sep 12:9:2058.|Front Immunol. 2021 May 7;12:667177.|Front Immunol. 2022 Oct 17:13:1007341.|Gene. 2018 Nov 30:677:149-162.|Int J Biol Sci. 2022 Jan 16;18 (4) :1363-1380.|J Allergy Clin Immunol. 2018 Jun;141 (6) :2286-2289.e5.|J Biomed Sci. 2025 Jan 6;32 (1) :5.|J Cell Mol Med. 2020 Jan;24 (2) :1588-1598.|J Cell Mol Med. 2020 Nov;24 (21) :12608-12618.|J Gastroenterol Hepatol. 2018 Feb;33 (2) :431-442.|J Immunol. 2018 Jul 15;201 (2) :814-820. |J Mol Cell Biol. 2023 Aug 3;15 (4) :mjad025.|J Mol Med (Berl) . 2019 Jan;97 (1) :25-35. |Johns Hopkins University. Department of Chemical and Biomolecular Engineering. 2016 Dec.|Karolinska Institutet. Dept of Physiology and Pharmacology. 2022 Feb.|Mol Biomed. 2025 Jun 10;6 (1) :40.|Mol Immunol. 2018 Sep:101:440-449.|Mol Ther. 2022 Nov 2;30 (11) :3430-3449.|Nat Commun. 2017 May 26;8:15584.|Oncogenesis. 2016 Jun 13;5 (6) :e234. |Oncotarget. 2017 Jul 21;8 (36) :60210-60222.|Oncotarget. 2018 Aug 24;9 (66) :32556-32569. |Patent. US20220251222A1.|Research Square Preprint. 2021 Mar.|Sci Adv. 2019 May 8;5 (5) :eaav7384.|Sci Rep. 2017 Nov 6;7 (1) :14510. |Stem Cells. 2015 Dec;33 (12) :3558-68. |University of Michigan. 2018 Oct.|Vet Immunol Immunopathol. 2016 Dec:182:52-58.|Xenotransplantation. 2018 Mar;25 (2) :e12385.|Ann Rheum Dis. 2016 Apr;75 (4) :721-9.|Biomed Res Int. 2020 Aug 5;2020:4670604.|bioRxiv. 2020 Sep 12:2020.08.25.265561.|Neurobiol Dis. 2021 Dec:160:105538.|Patent. US20170105971A1.|Patent. US20170181987A1.|Patent. US20240295544A1.

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