IA-14069
Based on 1 Customer Validation
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).
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- Pureté : 99.93%
- CAS No.: 2271216-04-5
- Formule: C20H15ClF2O4
- Masse moléculaire:392.78
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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. Further protocols information, click here.
In Vivo
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.
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Animal Model:TNF-α-transgenic (TNF-α-TG) Rheumatoid arthritis (RA) mice[1]
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Dosage:3.3, 33 mg/kg
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Administration:oral administration (p.o.), twice per week
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Result:Significantly reduced arthritis scores in TNF-α-TG mice.
Exerted dose-dependent preventive effects against RA development.
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Animal Model:TNF-α-transgenic (TNF-α-TG) RA mice[1]
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Dosage:25, 50, 100 mg/kg
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Administration:oral gavage (p.o.), 3 times per week
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Result:Effectively alleviated established arthritis in a dose-dependent manner, with higher doses exerting more potent therapeutic effects.
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Animal Model:Collagen-induced arthritis (CIA) RA mice[1]
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Dosage:25 mg/kg
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Administration:oral gavage (p.o.), 3 times per week
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Result:Exhibited notable therapeutic efficacy.
Lowered arthritis scores, mirroring the efficacy of the positive control Tofacitinib (HY-40354).
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Animal Model:Collagen-induced arthritis (CIA) RA mice[1]
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Dosage:10 mg/kg
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Administration:oral gavage (p.o.), 3 times per week
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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.
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Animal Model:C57BL/6 mice (21-23g) with DSS-induced (2-2.5 %, 5 days) acute colitis[2]
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Dosage:20, 40, 80, 160 mg/kg
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Administration:oral gavage (p.o.), daily for 5-12 days
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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).
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. 2271216-04-5
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Appearance Solid
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Masse moléculaire 392.78
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Formule C20H15ClF2O4
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Color White to off-white
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SMILES
O=C(C1=C(C2=C(F)C=CC(F)=C2)OC3=CC(Cl)=CC=C3C1=O)OC(C)(C)C
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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
Solvant et solubilité
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)
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)
Protocole
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
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TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
IA-14069 Related Classifications
HY-163102 Related Classifications
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