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| 10mg |
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| 25mg |
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Purity: ≥98%
Reparixin L-lysine salt, the L-lysine salt form of reparixin, is a novel, potent small molecule weight allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. It is the first medication candidate that is presently being studied in a clinical setting to prevent organ transplant recipients from suffering from ischemia/reperfusion injury. A computer-aided design program for dual allosteric CXCR1 and CXCR2 inhibitors has been developed using the binding mode of reparixin to CXCR1. Repertaxin and CXCR1 interact through a noncompetitive allosteric mode that locks CXCR1 in an inactive conformation to stop signaling, according to structural and biochemical data. In vivo, repertaxin effectively inhibits the recruitment of polymorphonuclear cells and shields organs from reperfusion injury. An overall tactic to control the activity of chemoattractant receptors is to target the Repertaxin interaction site of CXCR1.
| Targets |
CXCR1 ( IC50 = 1 nM ); CXCR2 ( IC50 ∼ 100 nM ); CXCR1Ile43Val ( IC50 = 80 nM ); CXCR1wtwt ( IC50 = 5.6 nM )
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| ln Vitro |
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| Enzyme Assay |
Reparixin L-lysine salt is a new and powerful small molecular weight allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. It is the L-lysine salt form of reparixin. Reparixin, as demonstrated in particular experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs, is a strong functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (about 400-fold) for CXCR1. Reparixin's effectiveness is considerably reduced in L1.2 cells that express the CXCR1 Ile43Val mutant (IC50 values for CXCR1 wt and CXCR1 Ile43Val, respectively, are 5.6 nM and 80 nM).
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| Cell Assay |
L1.2 Cell suspension (1.5-3×106 cells/mL) is then seeded in triplicate in the upper compartment of the chemotactic chamber after being incubated for 15 min at 37°C with either vehicle or Reparixin (1 nM-1μM). The following concentrations of various agonists are seeded in the chamber's lower compartment: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, and 30 nM C5a. The chemotactic chamber is incubated for 45 minutes (human PMNs) or 2 hours (monocytes) at 37°C in air with 5% CO2. After the incubation period, the filter is taken out, cleaned, and stained. Five oil immersion fields are counted for each migration at a high magnification of 100×, following sample coding. Transwell filters with a pore size of 5 μm are used to assess L1.2 migration.
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| Animal Protocol |
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| References |
| Molecular Formula |
C₂₀H₃₅N₃O₅S
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| Molecular Weight |
429.57
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| Exact Mass |
489.25
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| Elemental Analysis |
C, 53.97; H, 8.03; N, 8.58; O, 22.87; S, 6.55
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| CAS # |
266359-93-7
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| Related CAS # |
Reparixin; 266359-83-5
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| Appearance |
Solid powder
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| SMILES |
C[C@H](C1=CC=C(C=C1)CC(C)C)C(=O)NS(=O)(=O)C.C(CCN)C[C@@H](C(=O)O)N
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| InChi Key |
JEJFWWFZAQBZMJ-GVKMLHTLSA-N
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| InChi Code |
InChI=1S/C14H21NO3S.C6H14N2O2/c1-10(2)9-12-5-7-13(8-6-12)11(3)14(16)15-19(4,17)18;7-4-2-1-3-5(8)6(9)10/h5-8,10-11H,9H2,1-4H3,(H,15,16);5H,1-4,7-8H2,(H,9,10)/t11-;5-/m10/s1
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| Chemical Name |
(2S)-2,6-diaminohexanoic acid;(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 40 mg/mL (93.12 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3279 mL | 11.6395 mL | 23.2791 mL | |
| 5 mM | 0.4656 mL | 2.3279 mL | 4.6558 mL | |
| 10 mM | 0.2328 mL | 1.1640 mL | 2.3279 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05496868 | Recruiting | Drug: Reparixin 600mg Other: Matching Placebo |
Acute Respiratory Distress Syndrome, Adult |
Dompé Farmaceutici S.p.A | February 7, 2023 | Phase 2 |
| NCT05254990 | Recruiting | Drug: Reparixin Other: Placebo |
Infectious Pneumonia Severe COVID-19 |
Dompé Farmaceutici S.p.A | April 6, 2022 | Phase 3 |
| NCT05835466 | Recruiting | Drug: reparixin | Myelofibrosis (PMF) Post Essential Thrombocythemia Myelofibrosis (ET-MF) |
Icahn School of Medicine at Mount Sinai |
June 27, 2023 | Phase 2 |
| NCT04878055 | Completed | Drug: Reparixin Other: Placebo |
Pneumonia, Viral | Dompé Farmaceutici S.p.A | February 14, 2021 | Phase 3 |
| NCT02370238 | Completed | Drug: paclitaxel Drug: Reparixin |
Metastatic Breast Cancer | Dompé Farmaceutici S.p.A | July 29, 2015 | Phase 2 |
 Effect of Repertaxin on CXCL8 activity and binding to cellular receptors.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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 Effect of Repertaxin on cell signaling activated by CXCL8.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
 In vivoefficacy of Repertaxin in inhibiting PMN recruitment in CLP.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
 Molecular modeling of Repertaxin interaction with CXCR1/CXCR2.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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 In vivoefficacy of Repertaxin in inhibiting PMN recruitment and tissue damage in RI.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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