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. 2016 Nov 30;174(10):977–989. doi: 10.1111/bph.13656

Table 2.

Low MW relaxin receptor agonist ML290

Molecular formula (MW) RXFP1 EC50 (μM; Max. Resp.) ATP Tox. EC50 (μM; Max. resp.) Aqueous kinetic solubility in PBS (pH = 7) Liver microsomal stability (t1/2 in min; at 2 μM) Plasma stability (% remaining after 2 h) PK t1/2 in mice (h) at 30 mg·kg−1 i.p.
μg·mL−1 μM M H M H Plasma Heart
C24H21F3N2O5S (506.5) 0.094 (98%) 9.4 (−85%) 3.5 7 122 161 99 100 8.5 7.5

H, human serum; M, mouse serum. For intraperitoneal injections (i.p.) in pharmacokinetics (PK) studies the following formulation was used: 10% NMP (N‐Methyl‐2‐pyrrolidone) + 10% SolutolHS15 + 10% PEG400 + 70% Saline.