Farglitazar

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MedKoo CAT#: 326989

CAS#: 196808-45-4

Description: Farglitazar, also known as GI-262570, is a PPAR-γ agonist potentially for the treatment of type 2 diabetes. GI262570 can increase water and sodium reabsorption in distal nephron by stimulating the ENaC and Na,K-ATPase system.


Chemical Structure

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Farglitazar
CAS# 196808-45-4

Theoretical Analysis

MedKoo Cat#: 326989
Name: Farglitazar
CAS#: 196808-45-4
Chemical Formula: C34H30N2O5
Exact Mass: 546.22
Molecular Weight: 546.623
Elemental Analysis: C, 74.71; H, 5.53; N, 5.12; O, 14.63

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Farglitazar; GI-262570; GI 262570; GI262570.

IUPAC/Chemical Name: (S)-2-((2-benzoylphenyl)amino)-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic acid

InChi Key: ZZCHHVUQYRMYLW-HKBQPEDESA-N

InChi Code: InChI=1S/C34H30N2O5/c1-23-29(36-33(41-23)26-12-6-3-7-13-26)20-21-40-27-18-16-24(17-19-27)22-31(34(38)39)35-30-15-9-8-14-28(30)32(37)25-10-4-2-5-11-25/h2-19,31,35H,20-22H2,1H3,(H,38,39)/t31-/m0/s1

SMILES Code: O=C(O)[C@H](CC1=CC=C(OCCC2=C(C)OC(C3=CC=CC=C3)=N2)C=C1)NC4=CC=CC=C4C(C5=CC=CC=C5)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 546.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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9: Spraggs C, McCarthy A, McCarthy L, Hong G, Hughes A, Lin X, Sathe G, Smart D, Traini C, Van Horn S, Warren L, Mosteller M. Genetic variants in the epithelial sodium channel associate with oedema in type 2 diabetic patients receiving the peroxisome proliferator-activated receptor gamma agonist farglitazar. Pharmacogenet Genomics. 2007 Dec;17(12):1065-76. PubMed PMID: 18004211.

10: Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ. Co-crystal structure guided array synthesis of PPARgamma inverse agonists. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18. PubMed PMID: 17533125.

11: Yang B, Chen L, Qian Y, Triantafillou JA, McNulty JA, Carrick K, Clifton LG, Han B, Geske R, Strum J, Brown KK, Stimpson SA, Pahel G. Changes of skeletal muscle adiponectin content in diet-induced insulin resistant rats. Biochem Biophys Res Commun. 2006 Mar 3;341(1):209-17. Epub 2006 Jan 9. PubMed PMID: 16414018.

12: Tenenbaum A, Motro M, Fisman EZ. Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: the bezafibrate lessons. Cardiovasc Diabetol. 2005 Sep 16;4:14. Review. PubMed PMID: 16168052; PubMed Central PMCID: PMC1236941.

13: Yang B, Lin P, Carrick KM, McNulty JA, Clifton LG, Winegar DA, Strum JC, Stimpson SA, Pahel GL. PPARgamma agonists diminish serum VEGF elevation in diet-induced insulin resistant SD rats and ZDF rats. Biochem Biophys Res Commun. 2005 Aug 19;334(1):176-82. PubMed PMID: 15993383.

14: Golfman LS, Wilson CR, Sharma S, Burgmaier M, Young ME, Guthrie PH, Van Arsdall M, Adrogue JV, Brown KK, Taegtmeyer H. Activation of PPARgamma enhances myocardial glucose oxidation and improves contractile function in isolated working hearts of ZDF rats. Am J Physiol Endocrinol Metab. 2005 Aug;289(2):E328-36. Epub 2005 Mar 29. PubMed PMID: 15797988.

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19: Heppner TJ, Bonev AD, Eckman DM, Gomez MF, Petkov GV, Nelson MT. Novel PPARgamma agonists GI 262570, GW 7845, GW 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries. Pharmacology. 2005 Jan;73(1):15-22. Epub 2004 Sep 27. PubMed PMID: 15452359.

20: Gardiner SM, Nunez DJ, Baer PG, Brown KK, Bennett T. Regional hemodynamic effects of the N-(2-benzoylphenyl)-L-tyrosine peroxisome proliferator-activated receptor-gamma ligand, GI 262570 [(S)-2-(2-benzoylphenylamino)-3-[4-[2-(5-methyl-2-phenyl-2-oxazol-4-yl)ethoxy]phe nyl]propionic acid], in conscious rats. J Pharmacol Exp Ther. 2004 Sep;310(3):1226-33. Epub 2004 May 4. PubMed PMID: 15126643.