Reparixin (Repertaxin)

製品コードS8640 バッチS864001

印刷

化学情報

Chemical Structure Synonyms DF 1681Y Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H21NO3S
分子量 283.39 CAS No. 266359-83-5
Solubility (25°C)* 体外 DMSO 56 mg/mL (197.6 mM)
Ethanol 56 mg/mL (197.6 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).
in vitro

Reparixin (Repertaxin) is a non-competitive allosteric blocker of CXCR1 and CXCR2 receptor activation, which inhibits intracellular signal pathways without affecting receptor bindings. It potently and selectively inhibits a wide range of biological activities that are induced by CXCL8 such as leukocytes recruitment and functional inflammatory reactions. However, this compound does not affect CXCR1/CXCR2 activation induced by other chemotactic factors, C5a, fMLP, CXCL12 or several other agonists of GPCRs. It can regulate the production of angiotensin II receptors, which may influence Ang II-induced hypertension[1]. Reparixin specifically blocks CXCR1/2-mediated mouse and human neutrophil migration in vitro without affecting other receptors. It inhibits CXCL8-induced neutrophil activation through human CXCR1 and human CXCR2 and blocks phosphorylation of downstream signalling molecules. This compound prevents the increase of intracellular free calcium, elastase release and production of reactive oxygen intermediates, but leaves phagocytosis of Escherichia coli bacteria unaffected[2].
in vivo

Reparixin (Repertaxin), an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, attenuates inflammatory responses in various injury models. It effectively decreases systolic blood pressure and increases the blood flow. The thoracic aorta wall thickness is significantly decreased in SHR-R (the reparixin-treated group) compared to SHR-N (normal saline-treated SHR)[1]. (SHR: Spontaneously hypertensive rats)

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HUVECs
濃度 1 μM
反応時間 30 min
実験の流れ

HUVECs are pretreated without or with reparixin (Repertaxin) (1 μM) for 30 min. After this compound is applied, cells were then treated with or without Ang II (100 nmol/l) or CXCL8 (100 ng/ml) for 2 h. After total RNA is isolated, real-time PCR was performed.
動物実験 動物モデル SHR rats
投薬量 5 mg/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/21212529/
  • https://pubmed.ncbi.nlm.nih.gov/18587419/
  • https://pubmed.ncbi.nlm.nih.gov/15282370/

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Induction of cell death by the CXCR2 antagonist SB225002 in colorectal cancer and stromal cells [ Biomed Pharmacother, 2025, 188:118203] PubMed: 40412356
Chromosomal instability shapes the tumor microenvironment of esophageal adenocarcinoma via a cGAS-chemokine-myeloid axis [ bioRxiv, 2025, 2025.05.06.652454] PubMed: 40654626
The lipid-metabolism enzyme ECI2 reduces neutrophil extracellular traps formation for colorectal cancer suppression [ Nat Commun, 2024, 15(1):7184] PubMed: 39169021
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Myeloid-derived suppressor cells attenuate the antitumor efficacy of radiopharmaceutical therapy using 90Y-NM600 in combination with androgen deprivation therapy in murine prostate tumors [ J Immunother Cancer, 2024, 12(4)e008760] PubMed: 38663936
Sequence of androgen receptor-targeted vaccination with androgen deprivation therapy affects anti-prostate tumor efficacy [ J Immunother Cancer, 2024, 12(5)e008848] PubMed: 38772685

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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