PG 116800  (Synonyms: PG 530742; PGE 530742; PGE 7113313)

PG 116800 (PGE 530742; PGE 7113313) is an orally active, selective and high-affinity inhibitor of MMP. PG 116800 acts as an inhibitor of ventricular remodeling, reduces left ventricular volumes and infarct zone collagen content, and improves ejection fraction. PG 116800 is generally well tolerated, but is associated with higher rates of arthralgia, joint stiffness, and dyspepsia. PG 116800 can be used for the research of myocardial infarction^[1][2].

PG 116800 exhibits high binding affinity for purified MMP-2, -3, -8, -9, -13, and -14, and low affinity for purified MMP-1 and -7^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PG 116800 (3 or 6 months) causes joint swelling and collagen accumulation in rats, with reversible effects following treatment discontinuation^[1].
PG 116800 (12 months) causes joint swelling, collagen accumulation, periosteal fibrous tissue proliferation, and bone resorption in dogs, with reversible effects following treatment discontinuation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

501.55

C₂₄H₂₇N₃O₇S

291533-11-4

Solid

White to off-white

OC(C(NS(=O)(C1=CC=C(NC(C2=CC=C(OC)C=C2)=O)C=C1)=O)CC#CCN3CCOCC3)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Krzeski P, et al. Development of musculoskeletal toxicity without clear benefit after administration of PG-116800, a matrix metalloproteinase inhibitor, to patients with knee osteoarthritis: a randomized, 12-month, double-blind, placebo-controlled study. Arthritis Res Ther. 2007;9(5):R109.  [Content Brief]

  [2]. Hudson MP, et al. Effects of selective matrix metalloproteinase inhibitor (PG-116800) to prevent ventricular remodeling after myocardial infarction: results of the PREMIER (Prevention of Myocardial Infarction Early Remodeling) trial. J Am Coll Cardiol. 2006 Jul 4;48(1):15-20.