AM095 sodium
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MedKoo CAT#: 406568

CAS#: 1345614-59-6 (sodium)

Description: AM095 is a potent LPA1 receptor antagonist because it inhibited 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, and exhibited no LPA1 agonism. Lysophosphatidic acid (LPA) is a bioactive phospholipid that signals through a family of at least six G protein-coupled receptors designated LPA1-6. LPA type 1 receptor (LPA1) exhibits widespread tissue distribution and regulates a variety of physiological and pathological cellular functions.


Chemical Structure

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AM095 sodium
CAS# 1345614-59-6 (sodium)

Theoretical Analysis

MedKoo Cat#: 406568
Name: AM095 sodium
CAS#: 1345614-59-6 (sodium)
Chemical Formula: C27H23N2NaO5
Exact Mass:
Molecular Weight: 478.47
Elemental Analysis: C, 67.78; H, 4.85; N, 5.85; Na, 4.80; O, 16.72

Size Price Shipping out time Quantity
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 850 2 Weeks
500mg USD 1750 2 Weeks
1g USD 2950 2 Weeks
2g USD 5250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

AM095 sodium, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 1345614-59-6 (sodium)   1228690-36-5 (free acid)    

Synonym: AM095 AM-095; AM 095; AM095 sodium.

IUPAC/Chemical Name: sodium (R)-2-(4'-(3-methyl-4-(((1-phenylethoxy)carbonyl)amino)isoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetate

InChi Key: BDKDADFSIDCQGB-GMUIIQOCSA-M

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

SMILES Code: O=C([O-])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.[Na+].

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 478.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Gaire BP, Sapkota A, Song MR, Choi JW. Lysophosphatidic acid receptor 1 (LPA1) plays critical roles in microglial activation and brain damage after transient focal cerebral ischemia. J Neuroinflammation. 2019 Aug 20;16(1):170. doi: 10.1186/s12974-019-1555-8. PMID: 31429777; PMCID: PMC6701099.

2: Wen J, Lin X, Gao W, Qu B, Zuo Y, Liu R, Yu M. Inhibition of LPA1 Signaling Impedes Conversion of Human Tenon's Fibroblasts into Myofibroblasts Via Suppressing TGF-β/Smad2/3 Signaling. J Ocul Pharmacol Ther. 2019 Jul/Aug;35(6):331-340. doi: 10.1089/jop.2018.0120. PMID: 31343394.

3: Lee JH, Sarker MK, Choi H, Shin D, Kim D, Jun HS. Lysophosphatidic acid receptor 1 inhibitor, AM095, attenuates diabetic nephropathy in mice by downregulation of TLR4/NF-κB signaling and NADPH oxidase. Biochim Biophys Acta Mol Basis Dis. 2019 Jun 1;1865(6):1332-1340. doi: 10.1016/j.bbadis.2019.02.001. Epub 2019 Feb 11. PMID: 30763641.

4: Srikanth M, Chew WS, Hind T, Lim SM, Hay NWJ, Lee JHM, Rivera R, Chun J, Ong WY, Herr DR. Lysophosphatidic acid and its receptor LPA1 mediate carrageenan induced inflammatory pain in mice. Eur J Pharmacol. 2018 Dec 15;841:49-56. doi: 10.1016/j.ejphar.2018.10.005. Epub 2018 Oct 12. PMID: 30321532.

5: Ninou I, Kaffe E, Müller S, Budd DC, Stevenson CS, Ullmer C, Aidinis V. Pharmacologic targeting of the ATX/LPA axis attenuates bleomycin-induced pulmonary fibrosis. Pulm Pharmacol Ther. 2018 Oct;52:32-40. doi: 10.1016/j.pupt.2018.08.003. Epub 2018 Sep 7. PMID: 30201409.

6: Szepanowski F, Szepanowski LP, Mausberg AK, Kleinschnitz C, Kieseier BC, Stettner M. Lysophosphatidic acid propagates post-injury Schwann cell dedifferentiation through LPA1 signaling. Neurosci Lett. 2018 Jan 1;662:136-141. doi: 10.1016/j.neulet.2017.10.023. Epub 2017 Oct 16. PMID: 29051083.

7: Carmona-Rosas G, Alfonzo-Méndez MA, Hernández-Espinosa DA, Romero-Ávila MT, García-Sáinz JA. A549 cells as a model to study endogenous LPA1 receptor signaling and regulation. Eur J Pharmacol. 2017 Nov 15;815:258-265. doi: 10.1016/j.ejphar.2017.09.013. Epub 2017 Sep 21. PMID: 28943105.

8: Aikawa S, Kano K, Inoue A, Aoki J. Proliferation of mouse endometrial stromal cells in culture is highly sensitive to lysophosphatidic acid signaling. Biochem Biophys Res Commun. 2017 Feb 26;484(1):202-208. doi: 10.1016/j.bbrc.2016.12.154. Epub 2017 Jan 7. PMID: 28073697.

9: Velasco M, O'Sullivan C, Sheridan GK. Lysophosphatidic acid receptors (LPARs): Potential targets for the treatment of neuropathic pain. Neuropharmacology. 2017 Feb;113(Pt B):608-617. doi: 10.1016/j.neuropharm.2016.04.002. Epub 2016 Apr 5. PMID: 27059127.

10: Lee JM, Park SJ, Im DS. Lysophosphatidylethanolamine increases intracellular Ca(2+) through LPA(1) in PC-12 neuronal cells. Biochem Biophys Res Commun. 2015 May 29;461(2):378-82. doi: 10.1016/j.bbrc.2015.04.042. Epub 2015 Apr 16. PMID: 25888792.

11: Park SJ, Lee KP, Im DS. Action and Signaling of Lysophosphatidylethanolamine in MDA-MB-231 Breast Cancer Cells. Biomol Ther (Seoul). 2014 Feb;22(2):129-35. doi: 10.4062/biomolther.2013.110. PMID: 24753818; PMCID: PMC3975480.

12: Im DS. Intercellular Lipid Mediators and GPCR Drug Discovery. Biomol Ther (Seoul). 2013 Nov;21(6):411-22. doi: 10.4062/biomolther.2013.080. PMID: 24404331; PMCID: PMC3879912.

13: Ruisanchez É, Dancs P, Kerék M, Németh T, Faragó B, Balogh A, Patil R, Jennings BL, Liliom K, Malik KU, Smrcka AV, Tigyi G, Benyó Z. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90. doi: 10.1096/fj.13-234997. Epub 2013 Nov 18. PMID: 24249637; PMCID: PMC3898652.

14: Castelino FV, Seiders J, Bain G, Brooks SF, King CD, Swaney JS, Lorrain DS, Chun J, Luster AD, Tager AM. 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. doi: 10.1002/art.30262. PMID: 21305523; PMCID: PMC3086986.

15: Swaney JS, 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. doi: 10.1124/jpet.110.175901. Epub 2010 Dec 15. PMID: 21159750.



Additional Information

  Related CAS#
1345614-59-6 (sodium salt); 1228690-36-5 (free acid).