Art. -Nr.: HY-134471

TNF-α-IN-2

Name: TNF-α-IN-2
Brand: MedChemExpress
SKU: HY-134471
Price: 780.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.2%
CAS. Nr.: 2074702-04-6
Formel: C₂₅H₂₁ClF₂N₆O
Molecular Weight:494.92

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TNF-α-IN-2 Chemical Structure

CAS. Nr.: 2074702-04-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CD40

25 nM (IC₅₀)

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

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.

In Vivo

TNF-α-IN-2 (5-25 mg/kg; p.o. 1 h before TNF stimulation) inhibits TNF-induced IL-6 in mice^[1].
? 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 t_1/2 (6.2 h), low CL (6.6 mL/min?kg), and V_ss (3.2 L/kg) in mice^[1].
? TNF-α-IN-2 (2 mg/kg; p.o.) exhibits good oral bioavailability (58%), C_max (0.47 μM), and AUC_tot (5.9 μM?h) in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female C57Bl/6 mice^[1]
Dosage:

5, 25 mg/kg
Administration:

P.o. 1 h prior to TNF stimulation
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

CAS. Nr. 2074702-04-6
Appearance Solid
Molecular Weight 494.92
Formel C₂₅H₂₁ClF₂N₆O
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

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

Phytomedicine

Baicalin and N-acetylcysteine regulate choline metabolism via TFAM to attenuate cadmium-induced liver fibrosis. [Abstract]

2024 Mar:125:155337. PMID: 38241915

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0205 mL

10.1026 mL

20.2053 mL

5 mM

0.4041 mL

2.0205 mL

4.0411 mL

10 mM

0.2021 mL

1.0103 mL

2.0205 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xiao HY, et, al. Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches. J Med Chem. 2020 Dec 1. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

TNF-α-IN-2

1 Cited Publications

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TNF-α-IN-2

Publications Citing Use of MedChemExpress (MCE) TNF-α-IN-2

Alle TNF Receptor Isoform-spezifische Produkte anzeigen