Apratastat
Based on 4 publication(s) in Google Scholar
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC). Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureté: 99.28%
- CAS No.: 287405-51-0
- Formule: C17H22N2O6S2
- Masse moléculaire:414.50
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Apratastat
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Activité biologique
Description
IC50 & Target
[1]|
MMP |
In Vitro
Apratastat (10 μM, 24 hours) inhibits expression of pro-inflammatory cytokines TNF-α and IL-6 in lung tissue samples[3]. Apratastat (10 μM, 24 hours) reduces ADAM17 activity and MCAM release in HUVEC[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC (human umbilical vein endothelial cells)
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Significantly inhibited ADAM17 at the protein level.
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Cell Line:Lung tissue samples
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Significantly reduced mRNA levels of TNF-α and IL-6.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Poly(I ) (HY-107202) and SARS-CoV-2 RBD-S protein-induced lung inflammation model in C57BL/6 mice[3]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), administered twice at 4 and 16 hours post-surgery
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Result:Significantly reduced neutrophil and macrophage numbers in lung tissue, improved lung tissue morphology.
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Animal Model:MC38 colorectal cancer cell xenograft model in C57BL/6 mice[4]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.), once daily for 14 days
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Result:Significantly inhibited tumor growth, reduced tumor angiogenesis and lymphangiogenesis.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 287405-51-0
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Appearance Solid
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Masse moléculaire 414.50
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Formule C17H22N2O6S2
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Color White to off-white
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SMILES
CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1
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Synonyms
TMI-005
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Targeting a disintegrin and metalloprotease (ADAM) 17-CD122 axis enhances CD8+ T cell effector differentiation and anti-tumor immunity. [Abstract]2024 Jun 26;9(1):152. PMID: 38918390 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
bioRxiv
Omicron Spike confers enhanced infectivity and interferon resistance to SARS-CoV-2 in human nasal tissue. [Abstract]2023 Oct 12:2023.05.06.539698. PMID: 37425811
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (241.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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 (6.03 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 (6.03 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81. [Content Brief]
[2]. Ieguchi K, et al. Savior or not: ADAM17 inhibitors overcome radiotherapy-resistance in non-small cell lung cancer. J Thorac Dis. 2016 Aug;8(8):E813-5. [Content Brief]
[3]. Lartey NL, et al. ADAM17/MMP inhibition prevents neutrophilia and lung injury in a mouse model of COVID-19. J Leukoc Biol. 2022 Jun;111(6):1147-1158. [Content Brief]
[4]. Stalin J, et al. Targeting of the NOX1/ADAM17 Enzymatic Complex Regulates Soluble MCAM-Dependent Pro-Tumorigenic Activity in Colorectal Cancer. Biomedicines. 2023 Nov 30;11(12):3185. [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 | 2.4125 mL | 12.0627 mL | 24.1255 mL | 60.3136 mL |
| 5 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL | 12.0627 mL | |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4125 mL | 6.0314 mL | |
| 15 mM | 0.1608 mL | 0.8042 mL | 1.6084 mL | 4.0209 mL | |
| 20 mM | 0.1206 mL | 0.6031 mL | 1.2063 mL | 3.0157 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4125 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0105 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6031 mL | 1.5078 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 1.2063 mL | |
| 60 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0052 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7539 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6031 mL |
Apratastat Related Classifications
HY-119307 Related Classifications
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