Reparixin (Synonyms: Repertaxin; DF 1681Y)

Name: Reparixin
Brand: MedChemExpress
SKU: HY-15251
Rating: 5.0 (56 reviews)

Cat. No.: HY-15251 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC₅₀s of 1 and 100 nM, respectively.

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

Reparixin Chemical Structure

CAS No. : 266359-83-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 140	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 140	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
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 56 publication(s) in Google Scholar

Other Forms of Reparixin:

Reparixin L-lysine salt In-stock
(Rac)-Reparixin Get quote

52 Publications Citing Use of MCE Reparixin

Proliferation Assay

: Reparixin 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 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 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 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CXCR Isoform Specific Products:

View All Isoforms

CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC₅₀s of 1 and 100 nM, respectively.

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)

Cellular Effect

Cell Line	Type	Value	Description	References
L1.2	IC₅₀	0.0056 μM Compound: raparixin	Inhibition of CXCL8-induced cell migration in L1.2 cells expressing CXCR1 by chemotaxis assay Inhibition of CXCL8-induced cell migration in L1.2 cells expressing CXCR1 by chemotaxis assay	[PMID: 17665889]
L1.2	IC₅₀	0.08 μM Compound: raparixin	Inhibition of CXCL8-induced cell migration in L1.2 cells expressing Ile43Val CXCR1 mutant by chemotaxis assay Inhibition of CXCL8-induced cell migration in L1.2 cells expressing Ile43Val CXCR1 mutant by chemotaxis assay	[PMID: 17665889]

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

Reparixin is an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, has been shown to attenuate inflammatory responses in various injury models. Spontaneously hypertensive rats (SHR) are administered a subcutaneous injection of Reparixin (5 mg/kg) daily for 3 weeks. Reparixin effectively decreases systolic blood pressure and increased the blood flow^[3]. Reparixin reduces the levels of IL-1β in the brain after middle cerebral artery occlusion/reperfusion (MCAo) in mice. Bars represent levels of IL-1β (pg/100 mg) measured by ELISA in the brain tissues of mice subjected or not (SHAM) to MCAo and pretreated with vehicle or Reparixin (30 mg/kg, s.c.)^[4].

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

Clinical Trial

Molecular Weight

283.39

Formula

C₁₄H₂₁NO₃S

CAS No.

266359-83-5

Appearance

Solid

Color

White to off-white

SMILES

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (352.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5287 mL	17.6435 mL	35.2871 mL
5 mM	0.7057 mL	3.5287 mL	7.0574 mL
10 mM	0.3529 mL	1.7644 mL	3.5287 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (8.82 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 (8.82 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 (8.82 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.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (8.82 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.82 mM); Suspended 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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (248 KB) RP-HPLC (228 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]. Kim HY, 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. 2011;34(1):120-7. [Content Brief]

[4]. Sousa LF, et al. Blockade of CXCR1/2 chemokine receptors protects against brain damage in ischemic stroke in mice. Clinics (Sao Paulo). 2013;68(3):391-4. [Content Brief]

[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]

[6]. Krishnamurthy A, et al. Identification of a novel chemokine-dependent molecular mechanism underlying rheumatoid arthritis-associated autoantibody-mediated bone loss. Ann Rheum Dis. 2016 Apr;75(4):721-9. [Content Brief]

[7]. Crespo J, et al. Human Naive T Cells Express Functional CXCL8 and Promote Tumorigenesis. J Immunol. 2018 Jul 15;201(2):814-820. [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-1μM) 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]^[4]	Rats^[3] The Reparixin-treated group contained 5 SHR (SHR-R), where equal numbers of normal saline-treated SHR (SHR-N) and WKY (WKY-N) served as controls. Eighteen-week-old SHR received a subcutaneous injection of Reparixin (5 mg/kg) once per day for 3 weeks. Reparixin effects on blood flow, blood pressure and body weight are measured before treatment and then weekly until 1 week after the final injection. The effect of Reparixin on the expression of hypertension-related mediators in thoracic aortas, as well as nitric oxide (NO) plasma levels, is examined 1 week after the final injection. Mice^[4] C57BL/6J mice (8-10 weeks old/20-25 g) are used. The subcutaneous administration of Reparixin (30 mg/kg) is performed 60 minutes before cerebral ischemia induction. The animals are divided into the following three experimental groups: Sham (i.e., the group in which the arteries are visualized, but there is no occlusion of the middle cerebral artery), Vehicle (i.e., the group pre-treated with the vehicle, phosphate buffer solution, 60 minutes before MCAo) and Reparixin (i.e., the group pre-treated with the drug 60 minutes before MCAo). To evaluate neurological signs secondary to MCAo, the animals are assessed with the SHIRPA battery 24 h after reperfusion. 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]. Kim HY, 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. 2011;34(1):120-7. [Content Brief] [4]. Sousa LF, et al. Blockade of CXCR1/2 chemokine receptors protects against brain damage in ischemic stroke in mice. Clinics (Sao Paulo). 2013;68(3):391-4. [Content Brief] [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] [6]. Krishnamurthy A, et al. Identification of a novel chemokine-dependent molecular mechanism underlying rheumatoid arthritis-associated autoantibody-mediated bone loss. Ann Rheum Dis. 2016 Apr;75(4):721-9. [Content Brief] [7]. Crespo J, et al. Human Naive T Cells Express Functional CXCL8 and Promote Tumorigenesis. J Immunol. 2018 Jul 15;201(2):814-820. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.5287 mL	17.6435 mL	35.2871 mL	88.2176 mL
	5 mM	0.7057 mL	3.5287 mL	7.0574 mL	17.6435 mL
	10 mM	0.3529 mL	1.7644 mL	3.5287 mL	8.8218 mL
	15 mM	0.2352 mL	1.1762 mL	2.3525 mL	5.8812 mL
	20 mM	0.1764 mL	0.8822 mL	1.7644 mL	4.4109 mL
	25 mM	0.1411 mL	0.7057 mL	1.4115 mL	3.5287 mL
	30 mM	0.1176 mL	0.5881 mL	1.1762 mL	2.9406 mL
	40 mM	0.0882 mL	0.4411 mL	0.8822 mL	2.2054 mL
	50 mM	0.0706 mL	0.3529 mL	0.7057 mL	1.7644 mL
	60 mM	0.0588 mL	0.2941 mL	0.5881 mL	1.4703 mL
	80 mM	0.0441 mL	0.2205 mL	0.4411 mL	1.1027 mL
	100 mM	0.0353 mL	0.1764 mL	0.3529 mL	0.8822 mL

Reparixin 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:

Reparixin266359-83-5Repertaxin DF 1681YCXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Reparixin (Synonyms: Repertaxin; DF 1681Y)

Customer Review

Other Forms of Reparixin:

Reparixin Related Antibodies

52 Publications Citing Use of MCE Reparixin

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 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Reparixin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report