Darglitazone

Modify Date: 2024-01-08 16:49:30

Darglitazone Structure
Darglitazone structure
Common Name Darglitazone
CAS Number 141200-24-0 Molecular Weight 420.48100
Density N/A Boiling Point N/A
Molecular Formula C23H20N2O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Darglitazone


Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research[1].

 Names

Name 5-[[4-[3-(5-methyl-2-phenyl-1,3-oxazol-4-yl)propanoyl]phenyl]methyl]-1,3-thiazolidine-2,4-dione
Synonym More Synonyms

 Darglitazone Biological Activity

Description Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research[1].
Related Catalog
Target

PPAR-γ

In Vitro 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[2].
In Vivo 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[1]. Animal Model: Male diabetic ob/ob mice[1] 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.
References

[1]. Rashmi Kumari, et al. The PPAR-gamma agonist, darglitazone, restores acute inflammatory responses to cerebral hypoxia-ischemia in the diabetic ob/ob mouse. J Cereb Blood Flow Metab. 2010 Feb;30(2):352-60.

[2]. A Camirand, et al. Thiazolidinediones stimulate uncoupling protein-2 expression in cell lines representing white and brown adipose tissues and skeletal muscle. Endocrinology. 1998 Jan;139(1):428-31.

 Chemical & Physical Properties

Molecular Formula C23H20N2O4S
Molecular Weight 420.48100
Exact Mass 420.11400
PSA 118.06000
LogP 4.63550
Storage condition -20℃

 Precursor & DownStream

Precursor  1

DownStream  0

 Synonyms

5-[[4-[3-(5-methyl-2-phenyl-4-oxazolyl)-1-oxopropyl]phenyl]methyl]-2,4-thiazolidinedione
Darglitazone
5-[4-[3-(2-phenyl-5-methyl-4-oxazolyl)propionyl]benzyl]thiazolidine-2,4-dione
5-<4-<3-(5-methyl-2-phenyl-4-oxazolyl)propionyl>-benzyl>thiazolidine-2,4-dione
Darglitazone [INN]
[3H]Darglitazone
5-[4-[3-(5-methyl-2-phenyloxazol-4-yl)propionyl]benzyl]-thiazolidine-2,4-dione
UNII-AVP9C03Z3K
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