A non-competitive allosteric inhibitor of IL-8/CXCL8 activation of CXCR1 and CXCR2 chemokine receptors (IC50s = 1 and 100 nM

Reparixin (L-Lysine salt) – 1 mg

Brand:
Cayman
CAS:
266359-93-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{28557} 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.{28557} 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.{28553} Reparixin blockade (100 nM) of CXCR1 depletes a cancer stem cell population in human breast cancer cell lines in vitro.{28554}  

 

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Description

A non-competitive allosteric inhibitor of IL-8/CXCL8 activation of CXCR1 and CXCR2 chemokine receptors (IC50s = 1 and 100 nM, respectively); blocks IL-8-induced leukocyte recruitment (IC50 = 1 nM) and other inflammatory responses, without affecting receptor activation induced by other CXCR1 and CXCR2 agonists; at 100 nM, depletes a cancer stem cell population in human breast cancer cell lines in vitro

Formal name: (αR)-α-methyl-4-(2-methylpropyl)-N-(methylsulfonyl)benzeneacetamide, L-lysine

Synonyms:  Repertaxin

Molecular weight: 429.6

CAS: 266359-93-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Cancer|Cancer Stem Cell Research||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cell Biology|Stem Cell Research||Research Area|Immunology & Inflammation|Innate Immunity

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