AM095
(Synonyms: 4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐,AM 095;AM-095) 目录号 : GC15220
A selective LPA1 receptor antagonist
Cas No.:1345614-59-6
Sample solution is provided at 25 µL, 10mM.
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AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively [1].
In vitro, AM095 has shown to inhibit LPA1-induced chemotaxis of both mouse LPA1/CHO cells and human A2058 melanoma cells with IC50 values of 0.78 μM and 0.23μM [1].
In vivo, AM095 could dose-dependently block LPA-induced histamine release with an ED50 value of 8.3 mg/kg in mice. Additionally, AM095 has been revealed to remarkably reduce the BALF collagen and protein with an ED50 value of 10 mg/kg in lungs. AM095 has also shown to decrease both macrophage and lymphocyte infiltration induced by bleomycin in mice [1].
References:
[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.
| Cell experiment: [1] | |
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Cell lines |
MDA-MB-231 cells and SK-OV3 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
500 nM, 5 min |
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Applications |
Cells were pretreated with AM-095 or vehicle for 5 min and then treated with 10 μM of LPE or LPA. AM-095 (500 nM) completely inhibited LPA-induced [Ca2+]i responses in both cell lines and LPE-induced [Ca2+]i responses in MDA-MB-231 cells. AM-095 (500 nM) did not affect LPE-induced [Ca2+] i responses in SK-OV3 cells. |
| Animal experiment : [2] | |
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Animal models |
Female CD-1 mice |
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Dosage form |
Oral administration, 1–30 mg/kg |
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Applications |
Mice received AM095 in a volume of 10 ml/kg 2 h before the intravenous LPA (300 μg/mouse) challenge. LPA stimulated histamine release in a dose-dependent manner, resulting in a nearly 14-fold stimulation at the highest concentration tested. AM095 dose-dependently inhibited histamine release with an ED50 of 8.3 mg/kg and a maximal reduction of 80% at a dose of 30 mg/kg. By plotting the percentage inhibition of histamine release versus AM095 plasma concentrations for each individual animal and assuming a maximum response of 80% we generated an EC50 of ~ 1.5 μM. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| Cas No. | 1345614-59-6 | SDF | |
| 别名 | 4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐,AM 095;AM-095 | ||
| 化学名 | sodium;2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate | ||
| 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+] | ||
| 分子式 | C27H23N2NaO5 | 分子量 | 478.47 |
| 溶解度 | ≥ 23.9 mg/mL in DMSO, ≥ 16.77 mg/mL in EtOH with ultrasonic | 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 | 2.09 mL | 10.45 mL | 20.9 mL |
| 5 mM | 0.418 mL | 2.09 mL | 4.18 mL |
| 10 mM | 0.209 mL | 1.045 mL | 2.09 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet