AGG-523
Based on 1 Customer Validation
AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC50 of <0.03 and 0.04 μM. AGG-523 also inhibits MMP-2, -8, 12 activity AGG-523 attenuates release of aggrecanase-generated ARG-aggrecan fragments into synovial fluid, reduces surgery-induced ARG-aggrecan release in rat joint models, and inhibits aggrecanase activity to slow cartilage degradation. AGG-523 can be used for the research of osteoarthritis.
For research use only. We do not sell to patients.
- Purity: 99.32%
- CAS No.: 920289-29-8
- Formula: C28H29FN2O4
- Molecular Weight:476.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ADAMTS4 <0.03 μM (IC50) |
ADAMTS5 0.04 μM (IC50) |
MMP-2 |
MMP-8 |
MMP-12 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats with osteoarthritis (male, ~300g)[1]
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Dosage:1000 mg/kg
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Administration:P.o.; twice a day; 2 days
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Result:Inhibited surgery-induced ARG-aggrecan release by 38% at 2 hours post-last dose.
Inhibited surgery-induced ARG-aggrecan release by 78% at 4 hours post-last dose.
Achieved complete inhibition of surgery-induced ARG-aggrecan release at 6 and 8 hours post-last dose, with ARG-aggrecan levels close to or lower than those in un-operated contralateral knees of vehicle-treated animals.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 920289-29-8
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Appearance Solid
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Molecular Weight 476.54
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Formula C28H29FN2O4
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Color White to off-white
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SMILES
FC(C=C1)=CC=C1CC(C)(C)NC([C@H](CCC(O)=O)NC(C2=CC=C(C3=CC=CC=C3)C=C2)=O)=O
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Synonyms
PF-5212371
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 200 mg/mL (419.69 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 5 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (275 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.0985 mL | 10.4923 mL | 20.9846 mL | 52.4615 mL |
| 5 mM | 0.4197 mL | 2.0985 mL | 4.1969 mL | 10.4923 mL | |
| 10 mM | 0.2098 mL | 1.0492 mL | 2.0985 mL | 5.2461 mL | |
| 15 mM | 0.1399 mL | 0.6995 mL | 1.3990 mL | 3.4974 mL | |
| 20 mM | 0.1049 mL | 0.5246 mL | 1.0492 mL | 2.6231 mL | |
| 25 mM | 0.0839 mL | 0.4197 mL | 0.8394 mL | 2.0985 mL | |
| 30 mM | 0.0699 mL | 0.3497 mL | 0.6995 mL | 1.7487 mL | |
| 40 mM | 0.0525 mL | 0.2623 mL | 0.5246 mL | 1.3115 mL | |
| 50 mM | 0.0420 mL | 0.2098 mL | 0.4197 mL | 1.0492 mL | |
| 60 mM | 0.0350 mL | 0.1749 mL | 0.3497 mL | 0.8744 mL | |
| 80 mM | 0.0262 mL | 0.1312 mL | 0.2623 mL | 0.6558 mL | |
| 100 mM | 0.0210 mL | 0.1049 mL | 0.2098 mL | 0.5246 mL |
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