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Table 3 Activation of human and zebrafish PXRs by xenobiotics and vitamins

From: Evolution of pharmacologic specificity in the pregnane X receptor

Cmp. # Compound hPXR Activity hPXR Efficacy zfPXR Activity zfPXR Efficacy Toxicity
MI1 Acetaminophen None   None   None
MI2 3-Aminobenzoic acid None   None   None
MI3 Benzo [a]pyren 4.75 0.55 4.00 0.06 100
MI4 n-Butyl-4-aminobenzoate 4.88 1.35 4.86 0.69 100
MI5 Butylbenzoate None   None   None
MI6 Caffeine None   None   None
MI7 Carbamazepine 4.20 0.37 None   200
MI8 Carbamazepine epoxide 4.09 0.57 None   200
MI9 β-Carotene 5.46 0.67 None   100
MI10 Chlorpyrifos 4.59 2.05 5.44 0.88 None
MI11 Chlorzoxazone None   None   500
MI12 Cyclosporine None   None   20
MI13 Ecdysone None   None   None
MI14 Ethyl-2-aminobenzoate None   None   None
MI15 Flurbiprofen 4.10 1.59 4.10 0.53 None
MI16 Folic acid None   None   None
MI17 Guggulsterone None   None   None
MI18 GW3965 None   None   10
MI19 Hyperforin 7.22 1.29 None   50
MI20 Mevastatin 5.23 0.51 None   15
MI21 Mycophenolic acid None   None   None
MI22 Nifedipine 5.33 0.41 4.91 0.99 50
MI23 Oxcarbazepine 4.74 0.35 ~4.70 ~0.30 200
MI24 Paclitaxel 4.92 0.13 None   100
MI25 Phenobarbital 3.43 1.19 3.49 0.10 None
MI26 Phenytoin 4.26 0.52 None   200
MI27 n-Propyl-4-hydroxybenzoate 4.51 0.32 4.28 0.31 100
MI28 Provitamin D3 None   None   10
MI29 Provitamin D2 None   None   20
MI30 Reserpine 4.91 0.72 None   50
MI31 Retinol 5.80 0.20 None   50
MI32 Rifampicin 7.00 1.00 None   200
MI33 SR12813 6.41 0.90 None   10
MI34 TCDD 7.17 1.78 6.32 6.17 10
MI35 TCPOBOP 5.25 0.66 None   200
MI36 T-0901317 7.66 1.24 None   100
MI37 α-Tocopherol ~4.30 ~0.25 None   100
MI38 β-Tocopherol 4.85 0.33 None   100
MI39 δ-Tocopherol 5.14 0.64 None   100
MI40 γ-Tocopherol None   None   100
MI41 1α,25-Dihydroxyvitamin D3 None   None   50
MI42 1α-Hydroxyvitamin D2 None   None   50
MI43 1α-Hydroxyvitamin D3 None   None   50
MI44 Vitamin K1 4.99 0.13 None   100
MI45 Vitamin K2 5.04 0.80 None   100
MI46 Vitamin K3 ~4.30 ~0.15 None   100
  1. Activities are in -log(EC50), with EC50 in molar units for the activation of human or zebrafish PXR. Efficacy is relative to 10 μM rifampicin (human PXR) or 20 μM 5α-androstan-3α-ol (zebrafish PXR) which are assigned an efficacy of 1.0. Toxicity is the lowest concentration in micromolar that produced significant toxicity in the HepG2 cells.