PD-166793
Based on 1 publication(s) in Google Scholar
PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.21%
- CAS. Nr.: 199850-67-4
- Formel: C17H18BrNO4S
- Molecular Weight:412.30
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) PD-166793
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Biologische Aktivität
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MMP-2 4 nM (IC50) |
MMP-3 7 nM (IC50) |
MMP-13 8 nM (IC50) |
MMP-1 6.0 μM (IC50) |
MMP-7 7.2 μM (IC50) |
MMP-9 7.9 μM (IC50) |
PD-166793 (0.1 μM) leads to a 20% inhibition of AMP deaminase (AMPD) activity in rat heart homogenates[2].
PD-166793 (100 μM; 36 h) significantly reduces MMP-9 activity in normal human cardiac fibroblasts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PD-166793 (5 mg/kg; oral gavage) exhibits superior pharmacokinetics (t1/2=43.6 h, Cmax=42.4 μg/mL, AUC0-∞=2822 μg h/mL) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (6 weeks) were induced chronic biventricular volume overload[3]
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Dosage:1 mg/kg
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Administration:Daily gavage beginning 2 weeks before surgery and continued until 8 weeks after surgery
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Result:Prevented ventricular dilatation and attenuated the hypertrophy typically induced by chronic volume overload.
Chemical Information
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CAS. Nr. 199850-67-4
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Appearance Solid
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Molecular Weight 412.30
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Formel C17H18BrNO4S
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Color White to pink
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SMILES
CC(C)[C@@H](C(O)=O)NS(=O)(C1=CC=C(C2=CC=C(Br)C=C2)C=C1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
ProNotch converts extracellular protease activity into programmable transcriptional outputs. [Abstract]2026 Jun 3:2026.06.01.728985. PMID: 42282718
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (242.54 mM; Need ultrasonic; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (274 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)
Verweise
[1]. O'Brien PM, et, al. Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors. J Med Chem. 2000 Jan 27;43(2):156-66. [Content Brief]
[2]. Kaludercic N, et, al. Inhibiting metalloproteases with PD 166793 in heart failure: impact on cardiac remodeling and beyond. Cardiovasc Ther. Spring 2008;26(1):24-37. [Content Brief]
[3]. Chancey AL, et, al. Effects of matrix metalloproteinase inhibition on ventricular remodeling due to volume overload. Circulation. 2002 Apr 23;105(16):1983-8. [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 |
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| DMSO | 1 mM | 2.4254 mL | 12.1271 mL | 24.2542 mL | 60.6355 mL |
| 5 mM | 0.4851 mL | 2.4254 mL | 4.8508 mL | 12.1271 mL | |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4254 mL | 6.0635 mL | |
| 15 mM | 0.1617 mL | 0.8085 mL | 1.6169 mL | 4.0424 mL | |
| 20 mM | 0.1213 mL | 0.6064 mL | 1.2127 mL | 3.0318 mL | |
| 25 mM | 0.0970 mL | 0.4851 mL | 0.9702 mL | 2.4254 mL | |
| 30 mM | 0.0808 mL | 0.4042 mL | 0.8085 mL | 2.0212 mL | |
| 40 mM | 0.0606 mL | 0.3032 mL | 0.6064 mL | 1.5159 mL | |
| 50 mM | 0.0485 mL | 0.2425 mL | 0.4851 mL | 1.2127 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0106 mL | |
| 80 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL | 0.7579 mL | |
| 100 mM | 0.0243 mL | 0.1213 mL | 0.2425 mL | 0.6064 mL |
PD-166793 Related Classifications
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