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.