AM095 |
| رقم الكتالوجGC15220 |
A selective LPA1 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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+] | ||
| Formula | C27H23N2NaO5 | M.Wt | 478.47 |
| الذوبان | ≥ 23.9 mg/mL in DMSO, ≥ 16.77 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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