Reparixin L-lysine salt (Synonyms: Repertaxin L-lysine salt)

Name: Reparixin L-lysine salt
Brand: MedChemExpress
SKU: HY-15252
Rating: 5.0 (56 reviews)

Cat. No.: HY-15252 Purity: 99.66%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Reparixin L-lysine salt Chemical Structure

CAS No. : 266359-93-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 30	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 384	In-stock	Estimated Time of Arrival: December 31
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Based on 56 publication(s) in Google Scholar

Other Forms of Reparixin L-lysine salt:

Reparixin In-stock

52 Publications Citing Use of MCE Reparixin L-lysine salt

Proliferation Assay

: Reparixin L-lysine salt purchased from MedChemExpress. Usage Cited in: Front Immunol. 17 October 2022.; In HL-1 cells, when DSS and Reparixin (100nM) are applied in combination, the high expression levels of NF-κB, COX-2, ICAM-1 and VCAM-1 induced by OGD/R are further inhibited compared with that of DSS alone.

: Reparixin L-lysine salt purchased from MedChemExpress. Usage Cited in: J Gastroenterol Hepatol. 2018 Feb;33(2):431-442. [Abstract]; The effects of TRAF2 overexpression with or without Reparixin (100 nM), or BAY 11-7082 (30 μM) on the migration and invasion of AGS cell are examined by transwell assay.

: Reparixin L-lysine salt purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 21;8(36):60210-60222. [Abstract]; Migration assay of MDA-MB-231 cells treated 0.1 uM of Reparixin in CM from fibroblasts or macrophages with TCM of MDA-MB-231 cells using the Oris Cell migration kit.

: Reparixin L-lysine salt purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2016 Jun 13;5(6):e234. [Abstract]; The effects of Reparixin (100 nM) on the migration of OLFM4-depleted gastric cancer cells are detected by transwell assay.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]^[5]

CXCR1^wt

5.6 nM (IC₅₀, in L1.2 cells)

CXCR1^Ile43Val

80 nM (IC₅₀, in L1.2 cells)

CXCR1

1 nM (IC₅₀, in cells)

CXCR2

∼100 nM (IC₅₀, 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 (IC₅₀ 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].

MedChemExpress (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 [¹⁴C]-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].

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

Clinical Trial

Molecular Weight

429.57

Formula

C₂₀H₃₅N₃O₅S

CAS No.

266359-93-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

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:

H₂O : 100 mg/mL (232.79 mM; Need ultrasonic)

DMSO : 100 mg/mL (232.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 40 mg/mL (93.12 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (256 KB) HNMR (252 KB) RP-HPLC (84 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40 [Content Brief]

[4]. Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE TREATMENT OF BONE LOSS AND/OR PAIN. US 20170105971 A1.

[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. [Content Brief]

Cell Assay ^[1]	L1.2 Cell suspension (1.5-3×10⁶ cells/mL) is incubated at 37°C for 15 min in the presence of vehicle or of Reparixin (1 nM-1 μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber. Different agonists are seeded in the lower compartment of the chamber at the following concentrations: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, 30 nM C5a. The chemotactic chamber is incubated at 37°C in air with 5% CO₂ for 45 min (human PMNs) or 2 h (monocytes). At the end of incubation, the filter is removed, fixed, and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding. L1.2 migration is evaluated using 5 μm pore size Transwell filters^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Rats and Dogs^[3] Male and female Sprague-Dawley CD (albino) rats and male Lister Hooded (partially pigmented) rats are used. Male and female beagle Dogs (age about 15 months, bodyweight range 8.3-9.4 kg at the time of dosing) are used. Rats and Dogs are dosed i.v. with repurified [¹⁴C]-Reparixin free acid and an equivalent quantity of L-lysine suitably radiodiluted with Reparixin L-lysine salt in a solution of sterile isotonic (0.9%, w/v) saline. Rats are dosed with a solution of total drug concentration 9 mg/mL at a dose volume of 5 mL/kg (30 mg free Reparixin /kg) by bolus injection into a caudal vein. Dogs are dosed with a solution of total drug concentration 100 mg/mL at a dose volume of 0.5 mL/kg (33 mg free Reparixin/kg) by bolus injection into a superficial forelimb vein. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [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. [Content Brief] [3]. Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40 [Content Brief] [4]. Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE TREATMENT OF BONE LOSS AND/OR PAIN. US 20170105971 A1. [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.3279 mL	11.6395 mL	23.2791 mL	58.1977 mL
	5 mM	0.4656 mL	2.3279 mL	4.6558 mL	11.6395 mL
	10 mM	0.2328 mL	1.1640 mL	2.3279 mL	5.8198 mL
	15 mM	0.1552 mL	0.7760 mL	1.5519 mL	3.8798 mL
	20 mM	0.1164 mL	0.5820 mL	1.1640 mL	2.9099 mL
	25 mM	0.0931 mL	0.4656 mL	0.9312 mL	2.3279 mL
	30 mM	0.0776 mL	0.3880 mL	0.7760 mL	1.9399 mL
	40 mM	0.0582 mL	0.2910 mL	0.5820 mL	1.4549 mL
	50 mM	0.0466 mL	0.2328 mL	0.4656 mL	1.1640 mL
	60 mM	0.0388 mL	0.1940 mL	0.3880 mL	0.9700 mL
	80 mM	0.0291 mL	0.1455 mL	0.2910 mL	0.7275 mL
	100 mM	0.0233 mL	0.1164 mL	0.2328 mL	0.5820 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Reparixin L-lysine salt Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Reparixin266359-93-7RepertaxinCXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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Reparixin L-lysine salt (Synonyms: Repertaxin L-lysine salt)

Customer Review

Other Forms of Reparixin L-lysine salt:

Reparixin L-lysine salt Related Antibodies

52 Publications Citing Use of MCE Reparixin L-lysine salt

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CXCR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Reparixin L-lysine salt Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Reparixin L-lysine salt Related Classifications

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