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Chemical Structure| 266359-83-5 Chemical Structure| 266359-83-5
Chemical Structure| 266359-83-5

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Reparixin

CAS No.: 266359-83-5

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

Synonyms: Repertaxin;DF 1681Y

4.5 *For Research Use Only !

Cat. No.: A730164 Purity: 99%

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Product Details of [ Reparixin ]

CAS No. :266359-83-5
Formula : C14H21NO3S
M.W : 283.39
SMILES Code : O=C(NS(=O)(C)=O)[C@H](C)C1=CC=C(CC(C)C)C=C1
Synonyms :
Repertaxin;DF 1681Y
MDL No. :MFCD18633292
InChI Key :KQDRVXQXKZXMHP-LLVKDONJSA-N
Pubchem ID :9838712

Safety of [ Reparixin ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Biological Activity

Target
  • CXCR1

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Mouse osteoclasts 1 μg/mL 4 days To investigate the effect of ACPA on CXCL1 release from mouse osteoclasts, results showed that ACPA significantly increased CXCL1 release. PMC4819624
mouse hepatocytes 20 ng/ml 3 hours To evaluate whether TNF α upregulates CXCR1 expression, results showed that hepatocytes from CXCR2-/- mice had marked expression of CXCR1 after 24 hours of recovery from TNF α stimulation. PMC3058860
mouse hepatocytes 0-10,000 ng/ml 24 hours To evaluate the effects of CXCR1 signaling on hepatocyte cell death and proliferation, results showed that IL-8 stimulated marked hepatocyte proliferation at doses as low as 10 ng/ml and induced modest toxicity at the highest dose (10,000 ng/ml). PMC3058860
Neutrophils 10^-6 M 20 minutes Inhibited neutrophil chemotaxis induced by the ILT luminal layer by 50% PMC2682614
SUM159 cells 100 nM 3 days A 5-fold reduction in the proportion of ALDEFLUOR+ cells was observed, indicating that Reparixin selectively reduced the breast cancer stem cell (CSC) population. PMC2810075
SUM159 cells 100 nM 5 days A massive decrease in cell viability was observed, with only 3% of cells remaining viable, indicating that Reparixin induced massive apoptosis. PMC2810075
HCC1954 cells 100 nM 5 days A significant decrease in cell viability was observed, indicating that Reparixin had a similar cytotoxic effect on HCC1954 cells. PMC2810075
human PMN 1 µM 4 hours To evaluate the effect of Reparixin on CXCL8-induced gene expression, results showed that Reparixin inhibited CXCL8-induced gene expression. PMC511013
L1.2 transfectants 1 µM To evaluate the effect of Reparixin on CXCL8-induced cell migration, results showed that Reparixin inhibited CXCL8-induced cell migration. PMC511013
Human donor neutrophils 250 mg/ml Reparixin inhibited NET formation induced by septic patient plasma, reducing NET formation and fibrin deposition in the lungs PMC8792833

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice Balb/c mice Subcutaneous injection 15 mg/kg every 3 days for 14 consecutive days Reparixin completely reversed the bone loss induced by ACPA. PMC4819614
Mice ACPA-induced pain model Subcutaneous injection 10 mg/kg Daily for 14 consecutive days To investigate the effect of Reparixin on ACPA-induced pain-like behavior, results showed that Reparixin partially reversed ACPA-induced mechanical hypersensitivity. PMC4819624
mice hepatic ischemia/reperfusion injury model intraperitoneal injection 30 mg/kg/day Twice daily for 6 days To evaluate the role of CXCR1 in liver recovery after hepatic ischemia/reperfusion injury, results showed that Reparixin treatment delayed liver recovery and increased hepatocellular necrosis. PMC3058860
Mice SPARC-null mouse model Intraperitoneal injection 30 mg/kg/day Twice daily for 6 days Chronic inhibition with reparixin alleviated low back pain behaviors and attenuated disc inflammation in SPARC-null mice. PMC6558025
Mice Prostate tumor model Subcutaneous injection 30 mg/kg started 24 hours after reperfusion, every 12 hours Improve the antitumor efficacy of the TRT→ADT combination by blocking CXCR2 PMC11043705
NOD/SCID mice human breast cancer xenografts subcutaneous injection 20 or 30 mg/kg 3 times per week for 8 weeks Reparixin treatment alone or in combination with docetaxel significantly reduced the ALDEFLUOR+ population and retarded tumor growth, reducing metastasis. PMC2810075
mice Cecal Ligation and Puncture (CLP) model subcutaneous injection 5 mg/kg Thrice a week for 3 weeks To evaluate the inhibitory effect of Reparixin on PMN recruitment in the CLP model, results showed that Reparixin significantly reduced PMN recruitment. PMC511013
C57BL/6 male mice Sepsis model induced by caecal ligation and puncture (CLP) or intraperitoneal injection of Escherichia coli K12 strain Subcutaneous injection 15 mg/kg twice daily for 28 days Reparixin reduced NET formation, multi-organ injury, and mortality in septic mice without impairing bacterial clearance PMC8792833

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01220856 Pancreatic Islet Transplantati... More >>on in Type 1 Diabetes Mellitus Less << PHASE2 COMPLETED 2013-04-30 University Hospital Carl Gusta... More >>v Carus Dresden, Dresden, 01307, Germany|Ospedale San Raffaele, Milan, 20132, Italy Less <<
NCT01861054 Breast Cancer PHASE2 TERMINATED 2016-03-01 Indiana University Simon Cance... More >>r Center, Indianapolis, Indiana, 46202-5289, United States|University of Kansas Cancer Center, 4350 Shawnee Mission Pkwy, Suite 1500, Mailstop 6004, Fairway, Kansas, 66205, United States|The Cancer Institute of New Jersey, New Brunswick, New Jersey, 08903, United States|Montefiore Medical Center, MMC Medical Park at Eastchester, Bronx, New York, 10461, United States|Weill Cornell Medical College, New York, New York, 10065, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111, United States|Magee-Womens Hospital, Pittsburgh, Pennsylvania, 15213, United States|Sara Cannon Research Institute, Nashville, Tennessee, 37203, United States|The Methodist Hospital Research Institute, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.64mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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