| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
AM095 sodium is a novel, potent and selective LPA1 receptor antagonist that inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 of 0.98 and 0.73 μM, respectively. It did not show agonism for LPA1. Bioactive phospholipid lysophosphatidic acid (LPA) communicates via the LPA1-6 family of G protein-coupled receptors, which consists of at least six receptors. The LPA type 1 receptor (LPA1) is widely distributed throughout tissues and is involved in the regulation of numerous physiological and pathological cellular processes.
| ln Vitro |
AM095 is a potent LPA1 receptor antagonist as it inhibits GTPγS binding to the membrane of Chinese hamster ovary (CHO) cells 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 human LPA1 GTPγS binding assay is comparable to our previously published compounds AM966 (IC50=0.98±0.17 μM) and Debio-0719 compound (IC50=0.60±0.04 μM) [1]. AM095 inhibits LPA-induced calcium flux in CHO cells stably transfected with human or mouse LPA1. The IC50 of AM095 antagonizing LPA-induced calcium flux in human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively [2].
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| ln Vivo |
AM095 has high oral bioavailability and a moderate half-life and is well tolerated at doses tested in rats and dogs after oral and intravenous administration. Following oral administration (10 mg/kg) to rats, AM095 plasma concentrations peaked at 2 hours with a Cmax of 41 μM and then decreased to 10 nM by 24 hours. After intravenous (2 mg/kg) administration, a Cmax of 12 μM was observed within 15 minutes, which also dropped to approximately 10 nM by 24 hours, with a t1/2 of 1.79 hours. In dogs, a single oral dose of 5 mg/kg produces a peak plasma concentration of 21 μM within 15 minutes of administration, which then decreases to 10 nM within 24 hours. In comparison, an intravenous dose of 2 mg/kg resulted in a Cmax of 11 μM within 15 minutes, which decreased to 15 nM within 8 hours, resulting in a t1/2 of 1.5 hours [1].
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| References |
[3]. Im DS. Intercellular Lipid Mediators and GPCR Drug Discovery. Biomol Ther (Seoul). 2013 Nov;21(6):411-22. doi: 10.4062/biomolther.2013.080. Review. |
| Molecular Formula |
C27H23N2NAO5
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|---|---|
| Molecular Weight |
478.471698045731
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| Exact Mass |
478.15
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| Elemental Analysis |
C, 67.78; H, 4.85; N, 5.85; Na, 4.80; O, 16.72
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| CAS # |
1345614-59-6
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| Related CAS # |
AM095 free acid; 1228690-36-5; 1345614-59-6 (sodium)
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| Appearance |
Solid powder
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| SMILES |
CC1=NOC(=C1NC(=O)O[C@H](C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)[O-].[Na+]
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| InChi Key |
BDKDADFSIDCQGB-GMUIIQOCSA-M
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| InChi Code |
InChI=1S/C27H24N2O5.Na/c1-17-25(28-27(32)33-18(2)20-6-4-3-5-7-20)26(34-29-17)23-14-12-22(13-15-23)21-10-8-19(9-11-21)16-24(30)31;/h3-15,18H,16H2,1-2H3,(H,28,32)(H,30,31);/q;+1/p-1/t18-;/m1./s1
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| Chemical Name |
sodium;2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate
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| Synonyms |
AM095 sodium; AM095; AM-095; AM 095
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~174.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (10.45 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0900 mL | 10.4500 mL | 20.9000 mL | |
| 5 mM | 0.4180 mL | 2.0900 mL | 4.1800 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0900 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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