PG 116800
Based on 1 Customer Validation
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.
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- Purity: 99.81%
- CAS No.: 291533-11-4
- 화학식: C24H27N3O7S
- 분자량:501.55
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 291533-11-4
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Appearance Solid
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분자량 501.55
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화학식 C24H27N3O7S
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Color White to off-white
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SMILES
OC(C(NS(=O)(C1=CC=C(NC(C2=CC=C(OC)C=C2)=O)C=C1)=O)CC#CCN3CCOCC3)=O
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Synonyms
PG 530742; PGE 530742; PGE 7113313
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 5 mg/mL (9.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9938 mL | 9.9691 mL | 19.9382 mL | 49.8455 mL |
| 5 mM | 0.3988 mL | 1.9938 mL | 3.9876 mL | 9.9691 mL |