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AM-095 free base

Potent LPA1 receptor antagonist CAS# 1228690-36-5

AM-095 free base

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Chemical structure

AM-095 free base

3D structure

Chemical Properties of AM-095 free base

Cas No. 1228690-36-5 SDF Download SDF
PubChem ID 46213949 Appearance Powder
Formula C27H24N2O5 M.Wt 456.49
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 67.3 mg/mL (147.43 mM; Need ultrasonic and warming)
Chemical Name 2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid
SMILES CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)O
Standard InChIKey LNDDRUPAICPXIN-GOSISDBHSA-N
Standard InChI InChI=1S/C27H24N2O5/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)/t18-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AM-095 free base

DescriptionAM095 is a potent antagonist of LPA1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively.
TargetsLPA1 receptor    
IC500.98 μM (recombinant human) 0.73 μM (recombinant mouse)     

Protocol

Kinase Assay [3]
Assays are conducted using both hLPA1/CHO and mLPA1/CHO cells. A cell pellet of hLPA1/CHO or mLPA1/CHO cells is resuspended in appr 20 mL of ice-cold membrane buffer containing 10 mM HEPES, pH 7.4, 1 mM dithiothreitol, and protease inhibitors. Cells are sonicated, and the cell lysate is centrifuged at 2000 rpm for 10 min at 4°C. The supernatant is further centrifuged at 25,000 rpm for 70 min at 4°C. The membrane pellet is resuspended in 5 mL of ice-cold membrane buffer and homogenized using a Potter-Elvehjem tissue grinder. Final protein concentration is determined using the Bradford Protein Assay Kit. Known amounts of AM095 (diluted in dimethyl sulfoxide) or vehicle (dimethyl sulfoxide) 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 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.

Animal Administration [3]
Mice underwent UUO or sham surgery to the left kidney. In brief, a longitudinal, upper left incision is performed to expose the left kidney. The renal artery is located and a 6/0 silk thread is passed between the artery and the ureter. The thread is looped around the ureter and knotted three times insuring full ligation of ureter. The kidney is returned to abdomen, the abdominal muscle is sutured, and the skin is closed with staples. The contralateral (right) kidney served as an uninjured control. AM095 (30 mg/kg) or vehicle (water) is given 1 to 4 h before UUO and then b.i.d. thereafter by oral gavage. After 8 days, mice are euthanized using inhaled CO2, and the kidneys are harvested and cut in half for histopathological and biochemical analysis of fibrosis. To assess fibrosis, half of the kidney is fixed in 10% neutral buffered formalin and stained using Masson's trichrome. The other half of the kidney is frozen at −80°C for subsequent biochemical analysis of collagen content.

References:
[1]. 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. [2]. Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90. [3]. Swaney, J. S., 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.

AM-095 free base Dilution Calculator

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AM-095 free base Molarity Calculator

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Preparing Stock Solutions of AM-095 free base

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1906 mL 10.9531 mL 21.9063 mL 43.8126 mL 54.7657 mL
5 mM 0.4381 mL 2.1906 mL 4.3813 mL 8.7625 mL 10.9531 mL
10 mM 0.2191 mL 1.0953 mL 2.1906 mL 4.3813 mL 5.4766 mL
50 mM 0.0438 mL 0.2191 mL 0.4381 mL 0.8763 mL 1.0953 mL
100 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.4381 mL 0.5477 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AM-095 free base

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.

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References on AM-095 free base

Synthesis of Cyano-Containing Phenanthridine Derivatives via Catalyst-, Base-, and Oxidant-Free Direct Cyanoalkylarylation of Isocyanides.[Pubmed:28362091]

J Org Chem. 2017 Apr 21;82(8):4444-4448.

An efficient catalyst-, base-, and oxidant-free direct cyanoalkylarylation of isocyanides with AIBN has been developed under mild conditions. This strategy provides an elusive and rapid access to a wide range of cyano-containing phenanthridine derivatives in good yields via a one-pot alkylation/cyclization radical-cascade process. The mild reaction conditions together with no need of any catalyst, base, or oxidant make this protocol environmentally benign and practical.

Stabilization and Structure of the cis Tautomer of a Free-Base Porphyrin.[Pubmed:28370984]

Angew Chem Int Ed Engl. 2017 Aug 14;56(34):10088-10092.

Single-crystal X-ray analysis of the beta-heptakis(trifluoromethyl)-meso-tetrakis(p-fluorophenyl)porphyrin, H2 [(CF3 )7 TpFPP], has revealed the first example of a stable cis tautomer of a free-base porphyrin, the long-postulated intermediate of porphyrin tautomerism. The stability of the unique molecule appears to reflect a dual origin: a strongly saddled porphyrin skeleton, which alleviates electrostatic repulsion between the two NH protons, and two polarization-enhanced, transannular N-HO-HN hydrogen bond chains, each involving a molecule of water. DFT calculations suggest that the observed tautomer has a lower energy than the alternative, doubly hydrated trans tautomer by some 8.3 kcal mol(-1) . A fascinating prospect thus exists that H2 [(CF3 )7 TpFPP]2 H2 O and cognate structures may act as supramolecular synthons, which, given their chirality, may even be amenable to resolution into optically pure enantiomers.

The Laparoscopically Harvested Omental Free Flap: A Compelling Option for Craniofacial and Cranial Base Reconstruction.[Pubmed:28321385]

J Neurol Surg B Skull Base. 2017 Apr;78(2):191-196.

Background Management of craniofacial and cranial base tumors is a challenge due to the anatomic intricacies associated with the calvarium, the pathological diversity of lesions that present, and the potential complications. Clinical outcomes in laparoscopically harvested omentum free flaps for cranial base and craniofacial reconstruction are presented in this paper, in the largest case series to date. Methods A retrospective single-center experience for over 10 years with laparoscopically harvested omentum flaps used to reconstruct craniofacial and cranial base defects. Results A total of 13 patients underwent craniofacial or cranial base reconstruction using laparoscopically harvested omentum free flaps. The mean patient age was 48 years. The anterior skull base represented the most common site of reconstruction. A total of 12 of the flaps survived (92%), with one flap failure due to infection. All patients demonstrated satisfactory aesthetic and functional outcomes. There were no perioperative or intra-abdominal complications. Conclusions The laparoscopically harvested omentum free flap is a safe and effective tool in the armamentarium of the reconstructive surgeon. It is the ideal option to treat complex, three-dimensional subcutaneous defects, such as those encountered in craniofacial and cranial base reconstruction. Its unique angiogenic and immunologic capacity makes it an excellent flap for the previously irradiated and/or infected wound bed.

Chiral Tertiary Sulfonium Salts as Effective Catalysts for Asymmetric Base-Free Neutral Phase-Transfer Reactions.[Pubmed:28371093]

Angew Chem Int Ed Engl. 2017 Apr 18;56(17):4819-4823.

Although chiral quaternary ammonium and phosphonium salts are commonly used for asymmetric organocatalysis, the catalytic ability of chiral tertiary sulfonium salts has yet to be demonstrated in asymmetric synthesis. Herein, we show that chiral bifunctional trialkylsulfonium salts catalyze highly enantioselective conjugate additions of 3-substituted oxindoles to maleimides under base-free neutral phase-transfer conditions.

Description

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

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