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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A413560-5mg | 5mg | In stock | $93.90 | |
A413560-10mg | 10mg | In stock | $147.90 | |
A413560-25mg | 25mg | In stock | $333.90 | |
A413560-50mg | 50mg | In stock | $444.90 | |
A413560-100mg | 100mg | In stock | $692.90 |
LPA Receptor Antagonists
Synonyms | [1,1'-Biphenyl]-4acetic acid,4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]- | 2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid | GTPL6988 | 1228690-36-5 | AC-35875 | CYCLOPENTASILOXAN |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of LPA 1 receptor |
Product Description | Information AM 095 AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. Targets LPA1 receptor In vitro 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. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). In vivo AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. It dose-dependently reduceS LPA-stimulated histamine release, attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and decreases kidney fibrosis in a mouse unilateral ureteral obstruction model. Despite its antifibrotic activity, AM095 has no effect on normal wound healing after incisional and excisional wounding in rats. |
ALogP | 5.284 |
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HBD Count | 1 |
Rotatable Bond | 8 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Pubchem Sid | 488201268 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488201268 |
IUPAC Name | 2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid |
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 |
InChi Key | LNDDRUPAICPXIN-GOSISDBHSA-N |
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 |
Isomeric 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 |
PubChem CID | 46213949 |
Molecular Weight | 456.49 |
PubChem CID | 46213949 |
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CAS Registry No. | 1228690-36-5 |
ChEMBL Ligand | CHEMBL2182052 |
GPCRdb Ligand | AM095 |
PubChem SID | 488201268 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C2321225 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321231 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321241 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321242 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321414 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321476 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321555 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321565 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321590 | Certificate of Analysis | Jan 16, 2023 | A413560 |
C2321591 | Certificate of Analysis | Jan 16, 2023 | A413560 |
Solubility | Solubility (25°C) In vitro DMSO: 91 mg/mL (199.34 mM); Ethanol: 3 mg/mL (6.57 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 91 |
DMSO(mM) Max Solubility | 199.347192709588 |
Water(mg / mL) Max Solubility | <1 |
Starting at $241.90