AM095
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AM095是新型的、有效的和口服的溶血磷脂酸受体1（LPA1）拮抗剂，对重组人和小鼠LPA1的IC50值分别为0.98和0.73 μM[1]。
在小鼠LPA1/CHO细胞和人A2058黑色素瘤细胞中，AM095体外抑制LPA1诱导的趋化性，其IC50值分别为0.78 μM和0.23μM[1]。
在小鼠体内，AM095剂量依赖性地阻断LPA诱导的组胺释放，其ED50值为8.3 mg/kg。此外，在肺部，AM095显著降低支气管肺泡灌洗液中的胶原和蛋白，其ED50值为10 mg/kg。在小鼠中，AM095也减少Bleomycin诱导的巨噬细胞和淋巴细胞浸润[1]。
参考文献：
[1] Swaney JS1, Chapman C, Correa LD, Stebbins KJ, Broadhead AR, Bain G, Santini AM, Darlington J, King CD, Baccei CS, Lee C, Parr TA, Roppe JR, Seiders TJ, Ziff J, Prasit P, Hutchinson JH, Evans JF, Lorrain DS. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.
- 1. Ingrid Lua, Steven Balog, et al. "Loss of lysophosphatidic acid receptor 1 in hepatocytes reduces steatosis via down-regulation of CD36." Prostaglandins Other Lipid Mediat. 2021 Oct;156:106577. PMID:34147666
- 2. Harper K, R Lavoie R, et al. "The Hypoxic Tumor Microenvironment Promotes Invadopodia Formation and Metastasis through LPA1 Receptor and EGFR Cooperation." Mol Cancer Res. 2018 Jun 4. pii:molcanres.0649.2017. PMID:29866927
- 3. Szepanowski F, Szepanowski LP, et al. "Lysophosphatidic acid propagates post-injury Schwann cell dedifferentiation through LPA(1) signaling. Neurosci Lett." 2017 Oct 16;662:136-141. PMID:29051083
- 4. Banks DB, Chan GN, et al. "Lysophosphatidic acid and amitriptyline signal through LPA1R to reduce P-glycoprotein transport at the blood-brain barrier." J Cereb Blood Flow Metab. 2018 May;38(5):857-868. PMID:28447863
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 478.47 |
| Cas No. | 1345614-59-6 |
| Formula | C27H23N2NaO5 |
| Synonyms | AM 095;AM-095 |
| Solubility | ≥23.9 mg/mL in DMSO; insoluble in H2O; ≥16.77 mg/mL in EtOH with ultrasonic |
| Chemical Name | sodium;2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate |
| SDF | Download SDF |
| Canonical SMILES | CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)[O-].[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
MDA-MB-231细胞和SK-OV3细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
|
反应条件 |
500 nM，5 min |
|
实验结果 |
用AM-095或载体预处理细胞5分钟，然后用10 μM LPE或LPA处理。AM-095（500 nM）完全抑制两种细胞系中LPA诱导的[Ca2+]i应答和MDA-MB-231细胞中LPE诱导的[Ca2+]i应答。AM-095（500 nM）不影响SK-OV3细胞中LPE诱导的[Ca2+]i应答。 |
| 动物实验[2]: | |
|
动物模型 |
雌性CD-1小鼠 |
|
剂量 |
口服，1–30 mg/kg |
|
实验结果 |
静脉内LPA（300 μg/mouse）攻击前2小时，给予小鼠10 ml/kg的AM095。LPA以剂量依赖性方式刺激组胺释放，在测试的最高浓度下引起接近14倍的刺激。AM095以剂量依赖性的方式抑制组胺释放，ED50为8.3 mg/kg，在30 mg/kg的剂量下最大减少80％。通过绘制组胺释放相对于每只动物的AM095血浆浓度的抑制百分比，假设最大响应为80％，我们计算得到EC50大约为1.5 μM。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Park S J, Lee K P, Im D S. Action and Signaling of Lysophosphatidylethanolamine in MDA-MB-231 Breast Cancer Cells. Biomolecules & therapeutics, 2014, 22(2): 129. [2] Swaney J S, Chapman C, Correa L D, et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics, 2011, 336(3): 693-700. | |
| Description | AM095是有效的LPA1受体拮抗剂，对重组人和小鼠LPA1的IC50值分别为0.98和0.73 μM。 | |||||
| 靶点 | LPA1 receptor | |||||
| IC50 | 0.98 μM (recombinant human) 0.73 μM (recombinant mouse) | |||||
质量控制和MSDS
- 批次:
化学结构
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