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.
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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]。
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Animal experiment [1]: |
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Animal models |
C57Bl/6NrJ mice (Female; 8-12 weeks age) |
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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. |
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Dosage form |
30 mg/kg；i.p |
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Applications |
ABR-238901 ameliorates septic cardiomyopathy. |
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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. |
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| 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 |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet