Repertaxin
- Product Name
- Repertaxin
- CAS No.
- 266359-83-5
- Chemical Name
- Repertaxin
- Synonyms
- CS-2395;DF 1681Y;Reparaxin;Reparixin;Repertaxin;REPARIXIN;DF 1681Y;DF 1681Y;REPERTAXIN;Reparixin (Repertaxin;Reparixin 266359-83-5;Reparixin, 10 mM in DMSO
- CBNumber
- CB82628350
- Molecular Formula
- C14H21NO3S
- Formula Weight
- 283.39
- MOL File
- 266359-83-5.mol
Repertaxin Property
- Melting point:
- 103-105℃
- Density
- 1.137±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Room Temperature
- solubility
- Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)
- pka
- 4.28±0.40(Predicted)
- form
- solid
- color
- White
- optical activity
- [α]/D -80 to -90°, c =1.0 in ethanol
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
N-Bromosuccinimide Price
- Product number
- 464610
- Product name
- Reparixin
- Packaging
- 1mg
- Price
- $319
- Updated
- 2021/12/16
- Product number
- R144575
- Product name
- Reparixin
- Packaging
- 25mg
- Price
- $545
- Updated
- 2021/12/16
- Product number
- CS-1379
- Product name
- Reparixin
- Purity
- 99.98%
- Packaging
- 2mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-1379
- Product name
- Reparixin
- Purity
- 99.98%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- orb546075
- Product name
- Reparixin
- Purity
- >98%
- Packaging
- 5mg
- Price
- $158.1
- Updated
- 2021/12/16
Repertaxin Chemical Properties,Usage,Production
Description
Reparixin (CAS 266359-83-5) is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors (IC50?= 1 and 100 nM, respectively). It blocks a number of activities related to IL-8 signaling, including leukocyte recruitment (IC50?= 1 nM) without affecting receptor activation induced by other CXCR1 and CXCR2 agonists.1?In spontaneously hypertensive rats, 5 mg/kg reparixin administered daily for three weeks was shown to reduce blood pressure by inhibiting hypertension-related mediators.2?It attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord.3?Reparixin blockade (100 nM) of CXCR1 has also been used to deplete a cancer stem cell population in human breast cancer cell lines?in vitro.4
Uses
Prevention of delayed graft function in solid organ transplant (CXCL8 inhibitor).
Uses
Reparixin is an inhibitor of CXCR1 and CXCR2 chemokine receptors. Functions as an agent that blocks a range of activities including leukocyte recruitment and IL-8 signaling.
Definition
ChEBI: Reparixin is a monoterpenoid.
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].
IC 50
CXCR1wt: 5.6 nM (IC50, in L1.2 cells); CXCR1Ile43Val: 80 nM (IC50, in L1.2 cells); CXCR1: 1 nM (IC50, in cells); CXCR2: ～100 nM (IC50, in cells)
References
[1] Non-competitive allosteric inhibitors of the inflammatory cytokine receptors CXCR1 and CXCR2: prevention of reperfusion injury
[2] HYE YOUNG KIM. Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats.[J]. Biological & pharmaceutical bulletin, 2011, 34 1: 120-127. DOI:10.1248/bpb.34.120
[3] ALFREDO GORIO. Reparixin, an inhibitor of CXCR2 function, attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 322 3: 973-981. DOI:10.1124/jpet.107.123679
[4] CHRISTOPHE GINESTIER. CXCR1 blockade selectively targets human breast cancer stem cells in vitro and in xenografts.[J]. Journal of Clinical Investigation, 2010, 120 2: 485-497. DOI:10.1172/jci39397
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Raw materials
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