ADAMTS-5-IN-2
Based on 1 Customer Validation
ADAMTS-5-IN-2 is an inhibitor of ADAMTS-5 (IC50: 9.6 μM) and BoNT/A LC (IC50: 0.71 μM). ADAMTS-5-IN-2 can be used in research related to botulism, osteoarthritis, and other conditions.
For research use only. We do not sell to patients.
- Purity: 98.73%
- CAS No.: 294648-66-1
- Formula: C17H15N3OS
- Molecular Weight:309.39
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Storage: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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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
ADAMTS-5-IN-2 (compound 25) potently inhibits the activity of recombinant botulinum neurotoxin serotype A light chain (BoNT/A LC) in an in vitro FRET enzyme activity assay, with an IC50 of 0.71 μM[1].
ADAMTS-5-IN-2 (compound 11) inhibits ADAMTS-5 activity in a cell-free FRET assay, with an IC50 of 9.6 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 294648-66-1
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Appearance Solid
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Molecular Weight 309.39
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Formula C17H15N3OS
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Color Light yellow to brown
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SMILES
O=C1NC2=C(C=C(CC)C=C2)C13SC(C4=CC=CC=C4)=NN3
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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 : 100 mg/mL (323.22 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: 2.5 mg/mL (8.08 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (8.08 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Bompiani KM, et al. High-Throughput Screening Uncovers Novel Botulinum Neurotoxin Inhibitor Chemotypes. ACS Comb Sci. 2016;18(8):461-474. [Content Brief]
[2]. Bursavich MG, et al. 5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2). Bioorg Med Chem Lett. 2007;17(20):5630-5633. [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 | 3.2322 mL | 16.1608 mL | 32.3217 mL | 80.8042 mL |
| 5 mM | 0.6464 mL | 3.2322 mL | 6.4643 mL | 16.1608 mL | |
| 10 mM | 0.3232 mL | 1.6161 mL | 3.2322 mL | 8.0804 mL | |
| 15 mM | 0.2155 mL | 1.0774 mL | 2.1548 mL | 5.3869 mL | |
| 20 mM | 0.1616 mL | 0.8080 mL | 1.6161 mL | 4.0402 mL | |
| 25 mM | 0.1293 mL | 0.6464 mL | 1.2929 mL | 3.2322 mL | |
| 30 mM | 0.1077 mL | 0.5387 mL | 1.0774 mL | 2.6935 mL | |
| 40 mM | 0.0808 mL | 0.4040 mL | 0.8080 mL | 2.0201 mL | |
| 50 mM | 0.0646 mL | 0.3232 mL | 0.6464 mL | 1.6161 mL | |
| 60 mM | 0.0539 mL | 0.2693 mL | 0.5387 mL | 1.3467 mL | |
| 80 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0101 mL | |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8080 mL |
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