Table 2.

Inhibition of NPA hydrolysis in hMGL lysates by PPARγ ligands

Compound	Structure	hMGL pI50[IC50 (µM)]	rat brain FAAH IC50 (µM)	PPARγ EC50 (µM) (h/m)
Troglitazone		5.94 ± 0.03 (1.2)	∼200 µMa	0.55/0.78b
Ciglitazone		5.60 ± 0.05 (2.5)	84 µMa	−/3c
Rosiglitazone		4.53 ± 0.04 (29)	∼200 µMa	0.043/0.076b
CAY 10415		4.31 ± 0.04 (49)
15-deoxy-Δ12,14-prostaglandin J2		4.32 ± 0.06 (48)	87 µMa	−/2d
CAY 10514		<4 (>100)		0.64/−e

The pI₅₀ values and hence IC₅₀ values were calculated from the raw data shown in Figure 1B, using hMGL lysates (catalogue no. #10008354) and 0.25 mM NPA.

^aThe FAAH data are for rat brain homogenates, 0.5 µM [³H]AEA as substrate, and an assay pH of 7.4, and are taken from Lenman et al. (2007). The PPARγ values for troglitazone, ciglitazone, rosiglitazone, 5-deoxy-Δ^12,14-prostaglandin J₂ and CAY10514 are for transactivation assays using human (h) or mouse (m) chimeric receptors and are from

^bWillson et al. (2000)

^cWillson et al. (1996)

^dKliewer et al. (1995))

^eCaijo et al. (2005).

Note that CAY10514 showed a low efficacy compared with rosiglitazone, which in the same study reported to have an EC₅₀ value of 0.004 µM. Comparable data are not (to our knowledge) reported for CAY10415. However, this compound increases insulin-stimulated inccorporation of [¹⁴C]acetate into lipid in differentiated mouse 3T3-L1 cells at 3–10 µM concentrations (Tanis et al., 1996).