Darglitazone

Research use only, not for human use.

Darglitazone is a potent, selective agonist of PPAR-γ with antidiabetic actions. Darglitazone is effective in controlling blood glucose and lipid metabolism.

Darglitazone is a potent, selective agonist of PPAR-γ with antidiabetic actions. Darglitazone is effective in controlling blood glucose and lipid metabolism.(In Vitro):In cell lines representing white (3T3-L1 and 3T3-F442A) and brown (HIB-1B) adipose tissues and skeletal muscle (L6), Darglitazone(30 μM) stimulated the expression of UCP2 gene probably via PPAR-γ and increased uncoupling protein 2 (UCP2) mRNA.(In Vivo):In male diabetic ob/ob mice, Darglitazone dramatically reduces the infarct size in the ob/ob mice at 24 h of recovery. Normalized blood glucose and reduced circulating triglycerides (TG) and very-low-density lipoproteins (VLDL) in diabetic ob/ob mice without having any effect in the nondiabetic mice. Darglitazone treatment restores acute cerebral inflammatory responses that were absent in the diabetic mice and profoundly improved their recovery from hypoxic-ischemic (H/I) insult.

In cell lines representing white (3T3-L1 and 3T3-F442A) and brown (HIB-1B) adipose tissues and skeletal muscle (L6), within 4 h of exposing these cells to 30 μM Darglitazone, there is an increase in uncoupling protein 2 (UCP2) mRNA which reached a plateau of 5-10 times the basal in about 8 h. Darglitazone can stimulate the expression of UCP2 gene probably via PPAR-γ.

Darglitazone treatment restores euglycemia and normalized elevated corticosterone, triglycerides, and very-low-density lipoprotein levels. Darglitazone dramatically reduces the infarct size in the ob/ob mice at 24?h of recovery. Darglitazone treatment restores acute cerebral inflammatory responses that were absent in the diabetic mice and profoundly improved their recovery from hypoxic-ischemic (H/I) insult. Animal Model:Male diabetic ob/ob mice Dosage:1?mg/kg Administration:Oral administration; daily; for 7 days Result:Normalized blood glucose and reduced circulating triglycerides (TG) and very-low-density lipoproteins (VLDL) in diabetic ob/ob mice without having any effect in the nondiabetic mice.

CP-86325

Metabolic Enzyme/Protease

PPAR

Bacterial

——

——

141200-24-0

420.48

C23H20N2O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (118.91 mM)

Cc1oc(nc1CCC(=O)c1ccc(CC2SC(=O)NC2=O)cc1)-c1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years