Ladarixin(Synonyms: DF 2156A free base)

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Ladarixin (Synonyms: DF 2156A free base) 纯度: 98.05%

Ladarixin (DF 2156A free base) 是一种具有口服活性的,非竞争性的 CXCR1CXCR2 的变构抑制剂。Ladarixin 可用于 COPD 和哮喘的研究。

Ladarixin(Synonyms: DF 2156A free base)

Ladarixin Chemical Structure

CAS No. : 849776-05-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2200 In-stock
5 mg ¥2000 In-stock
10 mg ¥3500 In-stock
25 mg ¥7000 In-stock
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100 mg   询价  

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生物活性

Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma[1].

体外研究
(In Vitro)

Ladarixin inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 (IC50 at 0.7 nM)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ladarixin (10 mg/kg; p.o. once a day) reduces allergic airway inflammation in a model of single OVA exposure. Ladarixin reduces allergic airway inflammation, remodeling, and bronchial hyperreactivity in a model of chronic OVA exposure[1].
Ladarixin (10 mg/kg; p.o. once a day for 8 days) reduces pulmonary inflammation and fibrosis induced by bleomycin in mice[1].
Ladarixin (10 mg/kg; p.o. once a day for 3 days) protects mice from cigarette smoke-induced exacerbation of influenza-A infection[1].
Ladarixin is also effective in decreasing CXCL8-induced polymorphonuclear leukocyte infiltration in several animal models without a significant dose-related reduction in systemic neutrophil counts[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice (cigarette smoke-induced exacerbation of Influenza-A infection model)[1]
Dosage: 10 mg/kg
Administration: P.o. once a day at days 2, 3 and 4 post-infection
Result: Significantly attenuated the exacerbation in lethality and respiratory changes noted in CSFlu group.

Clinical Trial

分子量

375.34

Formula

C11H12F3NO6S2

CAS 号

849776-05-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (266.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6643 mL 13.3213 mL 26.6425 mL
5 mM 0.5329 mL 2.6643 mL 5.3285 mL
10 mM 0.2664 mL 1.3321 mL 2.6643 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 10 mg/mL (26.64 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Matheus Silverio Mattos, et al. CXCR1 and CXCR2 Inhibition by Ladarixin Improves Neutrophil-Dependent Airway Inflammation in Mice. Front Immunol. 2020 Oct 2;11:566953.

    [2]. Daria Marley Kemp, et al. Ladarixin, a dual CXCR1/2 inhibitor, attenuates experimental melanomas harboring different molecular defects by affecting malignant cells and tumor microenvironment. Oncotarget. 2017 Feb 28;8(9):14428-14442

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