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In vitro functional and pharmacokinetic properties of 13 diastereomersα
| Cpd | Structure | EC50 (nM) Mfn1 KO | EC50 (nM) Mfn2 KO | hPPB (%) | mPPB (%) | t1/2 HLM (min) | t1/2 MLM (min) | PAMPA-BBB Pe (nm/sec) |
|---|---|---|---|---|---|---|---|---|
| 13A |  |
inactive | inactive | 93.9 | 93.8 | 102 | 70 | 42.6 |
| 13B |  |
9.53 (6.35–14.02) | 7.69 (5.40–10.74) | 90.4 | 96.7 | >145 | 127 | 22.9 |
EC50 values are mean with 95% confidence limits.
