AM095
Based on 13 publication(s) in Google Scholar
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
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- Pureza: 99.72%
- No. CAS: 1345614-59-6
- Fòrmula: C27H23N2NaO5
- Peso molecular:478.47
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) AM095
More- Cell Commun Signal. 2023 Sep 25;21(1):257. [Abstract]
- EBioMedicine. 2020 Feb;52:102652. [Abstract]
- Mol Metab. 2023 Jun:72:101713. [Abstract]
- Front Aging Neurosci. 2022 Nov 16:14:1004002. [Abstract]
- Mol Pharm. 2023 Nov 6;20(11):5500-5514. [Abstract]
- Biomol Ther (Seoul). 2017 Mar 1;25(2):194-201. [Abstract]
- Biomol Ther (Seoul). 2014 Feb;22(2):129-35. [Abstract]
- Placenta. 2025 Aug:168:219-231. [Abstract]
- Vet Microbiol. 2021 Oct:261:109177. [Abstract]
- Biochem Biophys Res Commun. 2015 May 29;461(2):378-82. [Abstract]
- The Ohio State University. 2025.
- Seoul National University. 2024 Feb.
- Research Square Preprint. 2021 Aug.
Customer Validation & Images
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Cell Proliferation/Viability Assay
Actividad biológica
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LPA1 Receptor |
AM095 is a potent LPA1 receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). The IC50 of AM095 in the human LPA1 GTPγS binding assay is comparable with that of our previously published compound AM966 (IC50=0.98±0.17 μM) and the Debio-0719 compound (IC50=0.60±0.04 μM)[1]. AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1345614-59-6
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Appearance Solid
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Peso molecular 478.47
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Fòrmula C27H23N2NaO5
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Color Light yellow to khaki
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SMILES
O=C(O[Na])CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4)C)=O)C(C)=NO3)C=C2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration. [Abstract]2023 Sep 25;21(1):257. PMID: 37749552 -
EBioMedicine
A SNP of bacterial blc disturbs gut lysophospholipid homeostasis and induces inflammation through epithelial barrier disruption. [Abstract]2020 Feb;52:102652. PMID: 32058942 -
Mol Metab
Orexin induces the production of an endocannabinoid-derived lysophosphatidic acid eliciting hypothalamic synaptic loss in obesity. [Abstract]2023 Jun:72:101713. PMID: 36977433 -
Front Aging Neurosci
Positive association between plasmatic levels of orexin A and the endocannabinoid-derived 2-arachidonoyl lysophosphatidic acid in Alzheimer's disease. [Abstract]2022 Nov 16:14:1004002. PMID: 36466600 -
Mol Pharm
Integration of an LPAR1 Antagonist into Liposomes Enhances Their Internalization and Tumor Accumulation in an Animal Model of Human Metastatic Breast Cancer. [Abstract]2023 Nov 6;20(11):5500-5514. PMID: 37844135 -
Biomol Ther (Seoul)
Calcium Signaling of Lysophosphatidylethanolamine through LPA1 in Human SH-SY5Y Neuroblastoma Cells. [Abstract]2017 Mar 1;25(2):194-201. PMID: 27302965 -
Biomol Ther (Seoul)
2014 Feb;22(2):129-35. PMID: 24753818
AM095 purchased from MedChemExpress. Usage Cited in: Biomol Ther (Seoul). 2014 Feb;22(2):129-35. [Abstract]
Efficacies of LPE- and LPA-induced Ca2+ responses as compared to digitonin in MDA-MB-231 and SK-OV3 cells are shown as histograms.
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Placenta
Upregulation of PLAAT3 in syncytiotrophoblast induces activation of neutrophils via LPA-LPAR5 axis in preeclampsia. [Abstract]2025 Aug:168:219-231. PMID: 40623340 -
Vet Microbiol
Lipid metabolism is a novel and practical source of potential targets for antiviral discovery against porcine parvovirus. [Abstract]2021 Oct:261:109177. PMID: 34391196 -
Biochem Biophys Res Commun
Lysophosphatidylethanolamine increases intracellular Ca(2+) through LPA(1) in PC-12 neuronal cells. [Abstract]2015 May 29;461(2):378-82. PMID: 25888792 -
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Solvente y solubilidad
DMSO : 83.33 mg/mL (174.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Saline
Solubility: 5 mg/mL (10.45 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Known amounts of AM095 (diluted in DMSO) or vehicle (DMSO) are added to 25 to 40 μg of hLPA1/CHO or mLPA1/CHO membranes and 0.1 nM [35S]-GTPγS in buffer (50 mM HEPES, 0.1 mM NaCl, 10 mM MgCl2, 50 μg/mL saponin, pH 7.5) containing 0.2% fatty acid-free human serum albumin and 5 μM GDP. To test for LPA1 antagonist activity, the ability of AM095 to inhibit GTPγS binding stimulated by 900 nM LPA (18:1) is measured. Alternatively, to test for agonist effects, the ability of AM095 to stimulate GTPγS binding in the absence of LPA is measured. Reactions are incubated for 30 min at 30°C, before harvesting membranes onto glass filter binding plates (UniFilter GF/B) and washing three times with cold buffer containing 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2 using a Brandel 96-tip cell harvester. Plates are dried and then cpm are evaluated by using a Packard TopCount NXT microplate scintillation counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Male Sprague-Dawley rats with surgically implanted jugular vein catheters (250-300 g) are used. In all studies, animals are fasted 15 to 24 h before dosing. For rats, AM095 is administered intraveneously at a dose of 2 mg/kg in 0.9% saline given as a 1 mL/kg bolus injection into the jugular vein. To determine oral exposure, AM095 is administered as a solution in 0.5% methylcellulose via an oral gavage at a dose of 10 mg/kg in a volume of 3 mL/kg. Blood samples (approximately 300 μL of total blood) are taken from each rat via the jugular vein catheter at times up to 24 h postdose (10-11 samples per animal) in potassium EDTA tubes. After each sampling, the catheter is flushed with an equivalent volume of saline. Plasma samples, prepared by centrifugation of whole blood, are stored frozen (−80°C) before analysis. AM095 is dosed intravenously at 2 mg/kg and orally at 5 mg/kg to male beagle dogs (n=3). Plasma samples are collected and analyzed for AM095 concentration by liquid chromatography/mass spectrometry.
Mice[2]
C57Bl/6 mice are administered the selective LPA1 antagonist AM095 by oral gavage (30 mg/kg) at time 0 and 8 h, and blood is collected by cardiac puncture under anesthesia in sodium EDTA tubes at 0, 4, 8, 9, 12 and 24 h. Plasma samples are stored at −40°C prior to analysis of AM095 concentrations by liquid chromatography/mass spectrometry (LC-MS/MS). Known amounts of AM095 are added to thawed mouse plasma to yield a concentration range from 0.8 to 4,000 ng/mL. Plasma samples are precipitated using acetonitrile containing the internal standard buspirone. The analyte mixture (10 μL) is injected using a Leap PAL autosampler. Calibration curves are constructed by plotting the peak-area ratio of analyzed peaks against known concentrations. The lower limit of quantitation is 1 ng/mL. The data are subjected to linear regression analysis with 1/x2 weighting. The pharmacokinetic parameters of AM095 are calculated by non-compartmental analysis using WinNonlin Professional. Cmax and time to Cmax (Tmax) are obtained directly from the measured data.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Swaney JS, et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. [Content Brief]
[2]. Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0900 mL | 10.4500 mL | 20.9000 mL | 52.2499 mL |
| 5 mM | 0.4180 mL | 2.0900 mL | 4.1800 mL | 10.4500 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0900 mL | 5.2250 mL | |
| 15 mM | 0.1393 mL | 0.6967 mL | 1.3933 mL | 3.4833 mL | |
| 20 mM | 0.1045 mL | 0.5225 mL | 1.0450 mL | 2.6125 mL | |
| 25 mM | 0.0836 mL | 0.4180 mL | 0.8360 mL | 2.0900 mL | |
| 30 mM | 0.0697 mL | 0.3483 mL | 0.6967 mL | 1.7417 mL | |
| 40 mM | 0.0522 mL | 0.2612 mL | 0.5225 mL | 1.3062 mL | |
| 50 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0450 mL | |
| 60 mM | 0.0348 mL | 0.1742 mL | 0.3483 mL | 0.8708 mL | |
| 80 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6531 mL | |
| 100 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5225 mL |
AM095 Related Classifications
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