ABR-238901
目录号 : GC63420
ABR-238901是S100A8/A9阻断剂,有效抑制了S100A8/A9与高级糖基化终产物受体(RAGE)以及Toll样受体4(TLR4)之间的相互作用。
Cas No.:1638200-22-2
Sample solution is provided at 25 µL, 10mM.
ABR-238901 is a newly developed blocker for S100A8/A9, which effectively inhibits the interaction between S100A8/A9 and the receptor for advanced glycation endproducts (RAGE) as well as toll-like receptor 4 (TLR4) [1-2].
ABR-238901(30 mg/kg;i.p) ameliorates septic cardiomyopathy in mice [3]. ABR-238901, administered at a dose of 10 mg/kg intraperitoneally, reduces neutrophil extracellular trap (NET) formation in abdominal sepsis by inhibiting S100A9[4]. In abdominal sepsis, ABR-238901 at doses of 30 mg/kg administered intraperitoneally reduced lung levels of MPO (a marker of neutrophil activation) by 74% [5]. In mice with multiple myeloma (MM), treatment with ABR-238901 at a dose of 30 mg/kg given orally daily for 5 days reduces angiogenesis in vivo[6]. Administering ABR-238901 at a dose of 30 mg/kg intraperitoneally for a short duration shifts the balance between inflammation and repair towards a reparatory environment in the ischemic myocardium [7].
References:
[1]. Zhu H, He M, et,al. Low-intensity pulsed ultrasound alleviates doxorubicin-induced cardiotoxicity via inhibition of S100a8/a9-mediated cardiac recruitment of neutrophils. Bioeng Transl Med. 2023 Jul 7;8(6):e10570. doi: 10.1002/btm2.10570. PMID: 38023700; PMCID: PMC10658545.
[2]. Mareş RG, Sabău AH, et,al. S100A8∕A9 is a valuable biomarker and treatment target to detect and modulate neutrophil involvement in myocardial infarction. Rom J Morphol Embryol. 2023 Apr-Jun;64(2):151-158. doi: 10.47162/RJME.64.2.04. PMID: 37518871; PMCID: PMC10520380.
[3]. Jakobsson G, Papareddy P, et,al. Therapeutic S100A8/A9 blockade inhibits myocardial and systemic inflammation and mitigates sepsis-induced myocardial dysfunction. Crit Care. 2023 Sep 29;27(1):374. doi: 10.1186/s13054-023-04652-x. PMID: 37773186; PMCID: PMC10540409.
[4]. Du F, Ding Z, et,al. S100A9 induces reactive oxygen species-dependent formation of neutrophil extracellular traps in abdominal sepsis. Exp Cell Res. 2022 Dec 15;421(2):113405. doi: 10.1016/j.yexcr.2022.113405. Epub 2022 Oct 31. PMID: 36328195.
[5]. Ding Z, Du F, et,al. Targeting S100A9 Reduces Neutrophil Recruitment, Inflammation and Lung Damage in Abdominal Sepsis. Int J Mol Sci. 2021 Nov 29;22(23):12923. doi: 10.3390/ijms222312923. PMID: 34884728; PMCID: PMC8658007.
[6]. De Veirman K, De Beule N, et,al. Extracellular S100A9 Protein in Bone Marrow Supports Multiple Myeloma Survival by Stimulating Angiogenesis and Cytokine Secretion. Cancer Immunol Res. 2017 Oct;5(10):839-846. doi: 10.1158/2326-6066.CIR-17-0192. Epub 2017 Sep 13. PMID: 28903971.
[7]. Marinković G, Koenis DS, et,al. S100A9 Links Inflammation and Repair in Myocardial Infarction. Circ Res. 2020 Aug 14;127(5):664-676. doi: 10.1161/CIRCRESAHA.120.315865. Epub 2020 May 21. PMID: 32434457.
ABR-238901是S100A8/A9阻断剂,有效抑制了S100A8/A9与高级糖基化终产物受体(RAGE)以及Toll样受体4(TLR4)之间的相互作用[1-2]。
ABR-238901(30 mg/kg;i.p)改善了小鼠的感染性心肌病[3]。ABR-238901以每公斤10毫克的剂量腹腔注射,通过抑制S100A9减少了腹部感染的中性粒细胞外网(NET)的形成[4]。在腹部感染中,ABR-238901以30 mg/kg剂量腹腔注射,将肺部MPO(中性粒细胞活化标志物)水平降低了74%[5]。在多发性骨髓瘤(MM)小鼠中,每日口服30 mg/kg 的ABR-238901治疗5天可降低体内血管生成[6]。腹腔注射30 mg/kg的ABR-238901,短期内改变了缺血性心肌组织中炎症修复平衡,使其向修复环境转变[7]。
Animal experiment [1]: |
|
Animal models |
C57Bl/6NrJ mice (Female; 8-12 weeks age) |
Preparation method |
5 mg/kg LPS was used to induce endotoxemia through intraperitoneal injection. Subsequently, mice were administered ABR-238901 or PBS intraperitoneally at a dose of 30 mg/kg at 0 h and 6 h post-LPS injection, respectively. |
Dosage form |
30 mg/kg;i.p |
Applications |
ABR-238901 ameliorates septic cardiomyopathy. |
References: [1]. Jakobsson G, Papareddy P, et,al. Therapeutic S100A8/A9 blockade inhibits myocardial and systemic inflammation and mitigates sepsis-induced myocardial dysfunction. Crit Care. 2023 Sep 29;27(1):374. doi: 10.1186/s13054-023-04652-x. PMID: 37773186; PMCID: PMC10540409. |
Cas No. | 1638200-22-2 | SDF | |
分子式 | C11H9BrClN3O4S | 分子量 | 394.63 |
溶解度 | DMSO : 33.33 mg/mL (84.46 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg |
1 mM | 2.534 mL | 12.6701 mL | 25.3402 mL |
5 mM | 0.5068 mL | 2.534 mL | 5.068 mL |
10 mM | 0.2534 mL | 1.267 mL | 2.534 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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