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MedKoo Cat#: 406568 | Name: AM095 sodium
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

AM095 sodium
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: 0.0000

Molecular Weight: 478.47

Elemental Analysis: C, 67.78; H, 4.85; N, 5.85; Na, 4.80; O, 16.72

Price and Availability

Size Price Availability Quantity
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
200mg USD 850.00 2 Weeks
500mg USD 1,750.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 5,250.00 2 Weeks
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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
More Info
  Related CAS# 1345614-59-6 (sodium salt); 1228690-36-5 (free acid).      
Product Data
Product Data
Instruction
View handling instruction
Biological target:
AM095 is a selective LPA1 receptor antagonist.
In vitro activity:
Furthermore, the addition of AM095 to the culture medium strongly attenuated LPA toxicity on SMNs (Figure 7F). mRNAlpa3 is less abundant than mRNAlpa1 in the hypoglossal nucleus (−59.4% ± 5.7%) of neonatal rats and in SMNs (−98.6% ± 0.1%). In addition, AM095 is 8-times more effective at lpa1 than lpa3, without significant antagonism against lpa2,4,5. Therefore, AM095 effects on MN IME and LPA-induced cytotoxicity would be mainly explained by lpa1 targeting, although involvement of another LPAR cannot be fully excluded. Reference: Neuropathol Appl Neurobiol. 2021 Jan 28. https://pubmed.ncbi.nlm.nih.gov/33508894/
In vivo activity:
In vehicle-treated tMCAO group, severe brain infarction was developed in both the cerebral cortex and striatum (30.99 ± 1.77%), which was markedly reduced by AM095 administration (19.15 ± 3.84%; Fig. 1a, b). Similarly, AM095 administration significantly improved neurological functions in ischemic mice compared with vehicle administration (Fig. 1c). In addition, AM095 administration 1 h prior to tMCAO challenge significantly prevented brain damage compared with vehicle administration as assessed by brain infarction (Additional file 2: Figure S2a, b) and neurological deficit score (Additional file 2: Figure S2c). These data demonstrate that pharmacological inhibition of LPA1 can reduce brain damage in tMCAO-challenged mice, clearly suggesting that LPA1 signaling contributes to brain damage in cerebral ischemia. Reference: J Neuroinflammation. 2019; 16: 170. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6701099/
Solvent mg/mL mM
Solubility
DMSO 83.3 174.16
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Gento-Caro Á, Vilches-Herrando E, García-Morales V, Portillo F, Rodríguez-Bey G, González-Forero D, Moreno-López B. Interfering with lysophosphatidic acid receptor edg2/lpa1 signalling slows down disease progression in SOD1-G93A transgenic mice. Neuropathol Appl Neurobiol. 2021 Jan 28. doi: 10.1111/nan.12699. Epub ahead of print. PMID: 33508894. 2. 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. 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.
In vitro protocol:
1. Gento-Caro Á, Vilches-Herrando E, García-Morales V, Portillo F, Rodríguez-Bey G, González-Forero D, Moreno-López B. Interfering with lysophosphatidic acid receptor edg2/lpa1 signalling slows down disease progression in SOD1-G93A transgenic mice. Neuropathol Appl Neurobiol. 2021 Jan 28. doi: 10.1111/nan.12699. Epub ahead of print. PMID: 33508894.
In vivo protocol:
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. 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.
1: 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. 2: Szepanowski F, Winkelhausen M, Steubing RD, Mausberg AK, Kleinschnitz C, Stettner M. LPA1 signaling drives Schwann cell dedifferentiation in experimental autoimmune neuritis. J Neuroinflammation. 2021 Dec 17;18(1):293. doi: 10.1186/s12974-021-02350-5. PMID: 34920725; PMCID: PMC8680309. 3: Naruse T, Otake H, Takahashi T. Effects of a lysophosphatidic acid receptor 1 antagonist on hypertensive renal injury in Dahl-Iwai salt-sensitive rats. J Pharmacol Sci. 2022 Aug;149(4):179-188. doi: 10.1016/j.jphs.2022.05.003. Epub 2022 May 13. PMID: 35717071. 4: 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. 5: 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. 6: 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. 7: 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. 8: Bhattarai S, Sharma S, Subedi U, Ara H, Shum A, Milena M, Bhuiyan MS, Kidambi S, Sun H, Miriyala S, Panchatcharam M. The ATX-LPA Axis Regulates Vascular Permeability during Cerebral Ischemic-Reperfusion. Int J Mol Sci. 2022 Apr 8;23(8):4138. doi: 10.3390/ijms23084138. PMID: 35456953; PMCID: PMC9024554. 9: 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. 10: Gento-Caro Á, Vilches-Herrando E, García-Morales V, Portillo F, Rodríguez- Bey G, González-Forero D, Moreno-López B. Interfering with lysophosphatidic acid receptor edg2/lpa1 signalling slows down disease progression in SOD1-G93A transgenic mice. Neuropathol Appl Neurobiol. 2021 Dec;47(7):1004-1018. doi: 10.1111/nan.12699. Epub 2021 Feb 10. PMID: 33508894. 11: Lee GH, Cheon J, Kim D, Jun HS. Lysophosphatidic Acid Promotes Epithelial- Mesenchymal Transition in Kidney Epithelial Cells via the LPAR1/MAPK-AKT/KLF5 Signaling Pathway in Diabetic Nephropathy. Int J Mol Sci. 2022 Sep 10;23(18):10497. doi: 10.3390/ijms231810497. PMID: 36142408; PMCID: PMC9500642. 12: 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. 13: 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. 14: Yonezu Y, Tanabe S, Misawa H, Muramatsu R. Lysophosphatidic acid stimulates pericyte migration via LPA receptor 1. Biochem Biophys Res Commun. 2022 Aug 27;618:61-66. doi: 10.1016/j.bbrc.2022.06.016. Epub 2022 Jun 8. PMID: 35716596. 15: 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. 16: 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. 17: Fernandes MF, Tomczewski MV, Duncan RE. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid. Int J Mol Sci. 2022 Apr 9;23(8):4163. doi: 10.3390/ijms23084163. PMID: 35456981; PMCID: PMC9025735. 18: Forte N, Fernández-Rilo AC, Palomba L, Marfella B, Piscitelli F, De Girolamo P, Di Costanzo A, Di Marzo V, Cristino L. Positive association between plasmatic levels of orexin A and the endocannabinoid-derived 2-arachidonoyl lysophosphatidic acid in Alzheimer's disease. Front Aging Neurosci. 2022 Nov 16;14:1004002. doi: 10.3389/fnagi.2022.1004002. PMID: 36466600; PMCID: PMC9710385. 19: Prakash E, Pavithra S, Kishor Kumar DG, Panigrahi M, Singh TU, Kumar D, Parida S. TXA2 mediates LPA1-stimulated uterine contraction in late pregnant mouse. Prostaglandins Other Lipid Mediat. 2023 Aug;167:106736. doi: 10.1016/j.prostaglandins.2023.106736. Epub 2023 Apr 14. PMID: 37062326. 20: 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.