Art. -Nr.: HY-163102

IA-14069

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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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Reinheit: 99.93%
CAS. Nr.: 2271216-04-5
Formel: C₂₀H₁₅ClF₂O₄
Molecular Weight:392.78

Speicherung:

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

IA-14069 Chemical Structure

CAS. Nr.: 2271216-04-5

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2271216-04-5
Appearance Solid
Molecular Weight 392.78
Formel C₂₀H₁₅ClF₂O₄
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
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

Lösungsmittel & Löslichkeit

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)

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

2.5460 mL

12.7298 mL

25.4595 mL

5 mM

0.5092 mL

2.5460 mL

5.0919 mL

10 mM

0.2546 mL

1.2730 mL

2.5460 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
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]. Park S, et al. THU0047 IA-14069, A NOVEL SMALL-MOLECULE INHIBITOR DIRECT-TARGETING TUMOR NECROSIS FACTOR-α, ATTENUATES COLLAGEN INDUCED ARTHRITIS. Annals of the Rheumatic Diseases. 2019, 78:291

[2]. Okki Cho, et al. TNF targeting small molecule attenuates colonic inflammation in acute DSS-induced colitis mice. The Journal of Immunology, Volume 202, Issue 1_Supplement, May 2019, Page 52.11

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	2.5460 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

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Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IA-14069 Related Classifications

HY-163102 Related Classifications