2. Apoptosis NF-κB
  3. TNF Receptor NF-κB
  4. IA-14069

IA-14069 is an orally active tumor necrosis factor-α (TNF-α) inhibitor. IA-14069 binds directly to TNF-α and TNF-α-triggered signaling (p-IκBα and NF-κB p65) activities. Additionally, IA-14069 exerts a suppressive effect on Dextran sodium sulfate (HY-116282C) (DSS)-induced colitis. IA-14069 can be used for the research of Rheumatoid arthritis (RA) and inflammatory bowel disease (IBD).

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

IA-14069

IA-14069 Chemical Structure

CAS No. : 2271216-04-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

IA-14069 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

IA-14069 is an orally active tumor necrosis factor-α (TNF-α) inhibitor. IA-14069 binds directly to TNF-α and TNF-α-triggered signaling (p-IκBα and NF-κB p65) activities. Additionally, IA-14069 exerts a suppressive effect on Dextran sodium sulfate (HY-116282C) (DSS)-induced colitis. IA-14069 can be used for the research of Rheumatoid arthritis (RA) and inflammatory bowel disease (IBD)[1][2].

In Vitro

IA-14069 potently inhibits both TNF-α-induced cytotoxicity (IC50 < 0.7 μM), which directly binds to TNF-α and TNF-α-triggered signaling (p-IκBα and NF-κB p65) activities[1].

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

IA-14069 Related Antibodies
In Vivo

IA-14069 (3.3-33 mg/kg twice per week or 25-100 mg/kg 3 times per week, p.o.) exhibits both preventive and therapeutic anti-rheumatoid arthritis effects respectively in TNF-α-transgenic (TNF-α-TG) models[1].
IA-14069 (25 mg/kg, 3 times per week, p.o.) exhibits therapeutic anti-rheumatoid arthritis effects in collagen-induced arthritis (CIA) models[1].
IA-14069 (10 mg/kg, 3 times per week, p.o.) exerts synergistic effects with Methotrexate (HY-14519) (MTX, 5 mg/kg, 3 times per week, p.o.) in the CIA therapeutic model[1].
IA-14069 exhibits significant bioavailability and shows no in vivo toxicity even at excessive doses[1].
IA-14069 (20-160 mg/kg, daily for 5-12 days, p.o.) exerts a suppressive effect on DSS-induced colitis[2].

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

Animal Model: TNF-α-transgenic (TNF-α-TG) Rheumatoid arthritis (RA) mice[1]
Dosage: 3.3, 33 mg/kg
Administration: oral administration (p.o.), twice per week
Result: Significantly reduced arthritis scores in TNF-α-TG mice.
Exerted dose-dependent preventive effects against RA development.
Animal Model: TNF-α-transgenic (TNF-α-TG) RA mice[1]
Dosage: 25, 50, 100 mg/kg
Administration: oral gavage (p.o.), 3 times per week
Result: Effectively alleviated established arthritis in a dose-dependent manner, with higher doses exerting more potent therapeutic effects.
Animal Model: Collagen-induced arthritis (CIA) RA mice[1]
Dosage: 25 mg/kg
Administration: oral gavage (p.o.), 3 times per week
Result: Exhibited notable therapeutic efficacy.
Lowered arthritis scores, mirroring the efficacy of the positive control Tofacitinib (HY-40354).
Animal Model: Collagen-induced arthritis (CIA) RA mice[1]
Dosage: 10 mg/kg
Administration: oral gavage (p.o.), 3 times per week
Result: Synergized with methotrexate (MTX, 5 mg/kg, 3 times per week, oral gavage (p.o.)) (HY-14519), as the combination resulted in significantly lower arthritis scores than either monotherapy.
Animal Model: C57BL/6 mice (21-23g) with DSS-induced (2-2.5 %, 5 days) acute colitis[2]
Dosage: 20, 40, 80, 160 mg/kg
Administration: oral gavage (p.o.), daily for 5-12 days
Result: Significantly inhibited the severity of colitis, loss of body weight, and colon shortening at a dose of 80 mg/kg.
Suppressed markedly mucosal damages and production of the proinflammatory cytokines (TNF, IFN-g, IL-6, IL-17 and IL-5).
Clinical Trial
Molecular Weight

392.78

Formula

C20H15ClF2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C2=C(F)C=CC(F)=C2)OC3=CC(Cl)=CC=C3C1=O)OC(C)(C)C
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 (254.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5460 mL 12.7298 mL 25.4595 mL
5 mM 0.5092 mL 2.5460 mL 5.0919 mL
View the 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.

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

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 2.5460 mL 12.7298 mL 25.4595 mL 63.6489 mL
5 mM 0.5092 mL 2.5460 mL 5.0919 mL 12.7298 mL
10 mM 0.2546 mL 1.2730 mL 2.5460 mL 6.3649 mL
15 mM 0.1697 mL 0.8487 mL 1.6973 mL 4.2433 mL
20 mM 0.1273 mL 0.6365 mL 1.2730 mL 3.1824 mL
25 mM 0.1018 mL 0.5092 mL 1.0184 mL 2.5460 mL
30 mM 0.0849 mL 0.4243 mL 0.8487 mL 2.1216 mL
40 mM 0.0636 mL 0.3182 mL 0.6365 mL 1.5912 mL
50 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2730 mL
60 mM 0.0424 mL 0.2122 mL 0.4243 mL 1.0608 mL
80 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7956 mL
100 mM 0.0255 mL 0.1273 mL 0.2546 mL 0.6365 mL
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IA-14069 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IA-140692271216-04-5IA14069IA 14069TNF ReceptorNF-κBTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBRheumatoid arthritistumor necrosis factor-αTNF-αinflammatorycytokinecolitisInhibitorinhibitorinhibit

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