TNF-α-IN-2
Based on 1 publication(s) in Google Scholar
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.2%
- No. CAS: 2074702-04-6
- Fòrmula: C25H21ClF2N6O
- Peso molecular:494.92
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TNF-α-IN-2
MoreVer todos los productos específicos de isoformas TNF Receptor
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Actividad biológica
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CD40 25 nM (IC50) |
TNF-α-IN-2 (compound 42) (30 min) inhibits the E-selectin expression induced by soluble TNFα in HUVECs, with an IC50 of 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? TNF-α-IN-2 (2-10 mg/kg; p.o. twice daily for 10 d) dose dependently reduces both the clinical score as well as the levels of inflammatory cytokines and leukocyte cell surface receptors in mice[1].
? TNF-α-IN-2 (0.5 mg/kg; i.v.) exhibits long t1/2 (6.2 h), low CL (6.6 mL/min?kg), and Vss (3.2 L/kg) in mice[1].
? TNF-α-IN-2 (2 mg/kg; p.o.) exhibits good oral bioavailability (58%), Cmax (0.47 μM), and AUCtot (5.9 μM?h) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57Bl/6 mice[1]
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Dosage:5, 25 mg/kg
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Administration:P.o. 1 h prior to TNF stimulation
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Result:Inhibited IL-6 moderately at 5 mg/kg while the inhibition at 25 mg/kg was similar to mouse Enbrel, which served as the positive control in the study.
Chemical Information
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No. CAS 2074702-04-6
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Appearance Solid
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Peso molecular 494.92
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Fòrmula C25H21ClF2N6O
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Color Light yellow to yellow
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SMILES
C[C@H](C1=CC(C#N)=CC=C1F)NC2=C(C(C)=NC3=CC(F)=C(C4=CN=C(C(C)(O)C)N=C4)N=C23)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Phytomedicine
Baicalin and N-acetylcysteine regulate choline metabolism via TFAM to attenuate cadmium-induced liver fibrosis. [Abstract]2024 Mar:125:155337. PMID: 38241915
Solvente y solubilidad
DMSO : 100 mg/mL (202.05 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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.0205 mL | 10.1026 mL | 20.2053 mL | 50.5132 mL |
| 5 mM | 0.4041 mL | 2.0205 mL | 4.0411 mL | 10.1026 mL | |
| 10 mM | 0.2021 mL | 1.0103 mL | 2.0205 mL | 5.0513 mL | |
| 15 mM | 0.1347 mL | 0.6735 mL | 1.3470 mL | 3.3675 mL | |
| 20 mM | 0.1010 mL | 0.5051 mL | 1.0103 mL | 2.5257 mL | |
| 25 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 30 mM | 0.0674 mL | 0.3368 mL | 0.6735 mL | 1.6838 mL | |
| 40 mM | 0.0505 mL | 0.2526 mL | 0.5051 mL | 1.2628 mL | |
| 50 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
| 60 mM | 0.0337 mL | 0.1684 mL | 0.3368 mL | 0.8419 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2526 mL | 0.6314 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2021 mL | 0.5051 mL |
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