LPA2 antagonist 58

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Chemical Structure : LPA2 antagonist 58

Catalog No.: PC-20462Not For Human Use, Lab Use Only.

LPA2 antagonist 58 is a highly potent and selective LPA2 receptor antagonist with pIC50 of 8.22 (hLPA2) and 8.19 (mLPA2), >1000-fold selectivity over LPA1 receptor.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LPA2 antagonist 58 is a highly potent and selective LPA2 receptor antagonist with pIC50 of 8.22 (hLPA2) and 8.19 (mLPA2), >1000-fold selectivity over LPA1 receptor.
LPA2 antagonist 58 also highly selective against LPA3 and LPA5 isoforms (pIC50 < 4.30 for both receptors).
LPA2 antagonist 58 exhibits free exposure in lung after oral administration.

Physicochemical Properties

M.Wt	656.80
Formula	C30H37FN8O4S2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	methyl (S)-(5-((4-(2-((8-(3-((dimethylamino)methyl)-4-fluorophenyl)quinazolin-4-yl)amino)propyl)piperazin-1-yl)sulfonyl)-4-methylthiazol-2-yl)carbamate

References

1. Armani E, et al. J Med Chem. 2023 Apr 5. doi: 10.1021/acs.jmedchem.2c02087.

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