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抑制剂/激活剂

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Navarixin SCH 527123; MK-7123

Navarixin (SCH 527123) 是一种有效的，具有口服活性的变构的 CXCR1 和 CXCR2 拮抗剂，对猕猴 CXCR1 的 Kd 值为 41 nM，对小鼠，大鼠和猕猴 CXCR2 的 Kd 值分别为 0.20 nM，0.20 nM 和 0.08 nM。

货号：
TK0369
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	473727-83-2
生物活性	Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
分子式	C21H23N3O5
分子量	397.42
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (202.15 mM; Need ultrasonic) H2O : 5 mg/mL (20.22 mM; ultrasonic and warming and heat to 60°C)
体内研究	Navarixin (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED50=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Navarixin (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED=1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50=0.1 mg/kg) induced by intratracheal (i.t.) LPS.
体外研究	Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells. Navarixin (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner.
文献	•Nat Immunol. 2019 Nov;20(11):1444-1455. •Nat Microbiol. 2017 May 15;2:17072. •Nat Commun. 2021 May 5;12(1):2547. •J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4. •Cell Death Dis. 2022 Jan 13;13(1):57. •Sci Rep. 2019 Dec 20;9(1):19500. •Mol Pain. 2017 Jan-Dec;13:1744806917730212. •PLoS One. 2021 Sep 29;16(9):e0237659. •J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:42-53. •J Hard Tissue Biol. 2020, 29(1):9-16. •Patent. US20200281878A1. •Patent. US20180235964A1. •Patent. US20180221312A1. •Patent. US20170181987A1. •University of Calgary. Dec.23. 2015.
纯度及产品资料	98%

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