Target Validation Information
TTD ID	T36557
Target Name	Peroxisome proliferator-activated receptor delta (PPARD)
Type of Target	Clinical trial
Drug Potency against Target	Netoglitazone	Drug Info	EC50 = 3000 nM	[2]
	L-165461	Drug Info	IC50 = 4 nM	[1]
	L-796449	Drug Info	IC50 = 6 nM	[1]
Action against Disease Model	Netoglitazone	Drug Info	Netoglitazone is a thiazolidinedione, which acts as either a full or partial PPAR-gamma agonist, or antagonist, in a cell type specific manner, The pro-adipocytic and anti-osteoblastic activities of netoglitazone were evaluated in vitro, using both U-33/gamma2 cells as a model of marrow mesenchymal cell differentiation under the control of PPAR-gamma2 and primary bone marrowcultures, and in vivo in C57BL/6 mice. In vitro, netoglitazone induced adipocyte and inhibited osteoblast formation in a PPAR-gamma2-dependent manner; however, it was 100-fold less effective than rosiglitazone. In vivo, the administration of netoglitazone at an effective hyperglycemic dose (10 microg/g body weight/day) did not result in trabecular bone loss. Bone quality parameters such as bone mineral density and bone microarchitecture were not affected in netoglitazone-treated animals. The observed lack of an in vivo effect of netoglitazone on bone was entirely consistent with its low anti-osteoblastic activity in vitro	[3]
References
REF 1	Phenylacetic acid derivatives as hPPAR agonists. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.
REF 2	Treatment of non-insulin-dependent diabetes mellitus. Expert Opin Investig Drugs. 2003 Apr;12(4):623-33.
REF 3	Netoglitazone is a PPAR-gamma ligand with selective effects on bone and fat. Bone. 2006 Jan;38(1):74-84.

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