1. Apoptosis
  2. TNF Receptor
  3. TNF-α-IN-2

TNF-α-IN-2 

Cat. No.: HY-134471 Purity: 98.12%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

TNF-α-IN-2 Chemical Structure

TNF-α-IN-2 Chemical Structure

CAS No. : 2074702-04-6

Size Price Stock Quantity
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 6200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

CD40

25 nM (IC50)

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].

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 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].

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.
Molecular Weight

494.92

Formula

C25H21ClF2N6O

CAS No.
SMILES

C[[email protected]](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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (202.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
TNF-α-IN-2
Cat. No.:
HY-134471
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