[CAS NO. 266359-93-7] ReparixinL-lysinesalt

Name: ReparixinL-lysinesalt
Brand: Arctom Scientific
SKU: AS420975

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PRODUCTS SPECIFICATIONS [266359-93-7]

Fulfillment

Catalog

AS420975

Brand

Arctom Scientific

CAS

266359-93-7

DESCRIPTION [266359-93-7]

Overview

MDL	-
Molecular Weight	429.57
Molecular Formula	C20H35N3O5S
SMILES	N[C@@H](CCCCN)C(O)=O.CS(=O)(NC([C@@H](C1=CC=C(CC(C)C)C=C1)C)=O)=O

For research use only. We do not sell to patients.

43 Publications Citing Use of MCE

Summary

Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 ( CXCR1/2 ) activation.

IC50 & Target

CXCR1 ^wt

5.6 nM (IC ₅₀ , in L1.2 cells)

CXCR1 ^Ile43Val

80 nM (IC ₅₀ , in L1.2 cells)

CXCR1

1 nM (IC ₅₀ , in cells)

CXCR2

∼100 nM (IC ₅₀ , in cells)

In Vitro

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 (IC ₅₀ 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [ ¹⁴ C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50 µg/mL, but lower at higher concentrations. Although radioactivity is rapidly distributed into rat tissues, V _ss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t _1/2 ~0.5 h) than in dogs (t _1/2 ~10 h) ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01861054	Dompé Farmaceutici S.p.A	Breast Cancer	February 2013	Phase 2
NCT05254990	Dompé Farmaceutici S.p.A	Infectious Pneumonia\|Severe COVID-19	April 6, 2022	Phase 3
NCT01220856	Dompé Farmaceutici S.p.A	Pancreatic Islet Transplantation in Type 1 Diabetes Mellitus	July 28, 2010	Phase 2
NCT00224406	Dompé Farmaceutici S.p.A	Ischemia-Reperfusion Injury\|Lung Transplantation	May 2005	Phase 2
NCT04794803	Dompé Farmaceutici S.p.A	Severe Pneumonia	May 5, 2020	Phase 2\|Phase 3
NCT04878055	Dompé Farmaceutici S.p.A	Pneumonia, Viral	February 14, 2021	Phase 3
NCT02370238	Dompé Farmaceutici S.p.A\|PRA Health Sciences	Metastatic Breast Cancer	July 29, 2015	Phase 2
NCT03031470	Dompé Farmaceutici S.p.A	Ischemia-reperfusion Injury in Liver Transplant\|Early Allograft Dysfunction	March 2015	Phase 2
NCT05212701	Dompé Farmaceutici S.p.A	Fatigue\|Locally Advanced or Metastatic Breast Cancer	April 19, 2022	Phase 2
NCT05496868	Dompé Farmaceutici S.p.A	Acute Respiratory Distress Syndrome, Adult	November 25, 2022	Phase 2
NCT01817959	Dompé Farmaceutici S.p.A	Islet Transplantation in Diabetes Mellitus Type 1	October 2012	Phase 3
NCT01967888	Dompé Farmaceutici S.p.A	Pancreatectomy for Chronic Pancreatitis	February 2014	Phase 2\|Phase 3
NCT00248040	Dompé Farmaceutici S.p.A	Ischemia-Reperfusion Injury\|Kidney Diseases	October 2005	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 100 mg/mL ( 232.79 mM ; Need ultrasonic)

DMSO : 100 mg/mL ( 232.79 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 40 mg/mL (93.12 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

* All of the co-solvents are available by MCE.