An allosteric inhibitor of CXCR1 and CXCR2
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Reparixin (L-Lysine salt)

Item No. 21492

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR)-α-methyl-4-(2-methylpropyl)-N-(methylsulfonyl)benzeneacetamide, L-lysine
CAS Number
266359-93-7
Synonyms
  • Repertaxin
Molecular Formula
C14H21NO3S • C6H14N2O2
Formula Weight
429.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: slightly solubleDMSO: 10 mg/mlEthanol: slightly solublePBS (pH 7.2): 10 mg/ml
λmax
202 nm
SMILES
CS(NC([C@H](C)C1=CC=C(CC(C)C)C=C1)=O)(=O)=O.OC([C@@H](N)CCCCN)=O
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
InChi Key
JEJFWWFZAQBZMJ-GVKMLHTLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

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    5 mg

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    10 mg

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    25 mg

    $212

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    Cayman Chemical
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    Product Description

    Reparixin is a non-competitive allosteric inhibitor of the activation of CXCR1 and CXCR2 chemokine receptors by IL-8 (IC50s = 1 and 100 nM, respectively).1 It blocks a range of activities related to IL-8 signaling, including leukocyte recruitment (IC50 = 1 nM) and other inflammatory responses, without affecting receptor activation induced by other CXCR1 and CXCR2 agonists.1 In spontaneously hypertensive rats, 5 mg/kg reparixin administered daily for three weeks reduces blood pressure by inhibiting hypertension-related mediators, IL-8, 12-lipoxygenase, and endothelin-1.2 Reparixin blockade (100 nM) of CXCR1 depletes a cancer stem cell population in human breast cancer cell lines in vitro.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. USA 101(32), 11791-11796 (2004).

    2. Kim, H.Y., Choi, J.H., Kang, Y.J., 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. 34(1), 120-127 (2011).

    3. Ginestier, C., Liu, S., Diebel, M.E., et al. CXCR1 blockade selectively targets human breast cancer stem cells in vitro and in xenografts. J. Clin. Invest. 120(2), 485-497 (2010).