1. Metabolic Enzyme/Protease
    Apoptosis
  2. RAR/RXR
    Apoptosis
  3. AGN194204

AGN194204 (Synonyms: IRX4204; NRX194204; VTP 194204)

Cat. No.: HY-13717
Handling Instructions

AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.

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

AGN194204 Chemical Structure

AGN194204 Chemical Structure

CAS No. : 220619-73-8

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Description

AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].

IC50 & Target[1][2]

RXRα

0.4 nM (Kd)

RXRβ

3.6 nM (Kd)

RXRγ

3.8 nM (Kd)

RXRα

0.2 nM (EC50)

RXRβ

0.8 nM (EC50)

RXRγ

0.08 nM (EC50)

In Vitro

AGN194204 (NRX194204; 0-100 nM; 24 hours; E, RAW cells) treatment blocks the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells[1].
AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells[1].

Apoptosis Analysis[1]

Cell Line: SK-BR-3 human breast cancer cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Induced apoptosis in lung and breast cancer cells.

Western Blot Analysis[1]

Cell Line: E, RAW cells
Concentration: 0 nM, 1 nM, 10 nM and 100 nM
Incubation Time: 24 hours
Result: Blocked the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells.
In Vivo

AGN194204 (NRX194204; 30-60 mg/kg; oral administration; daily; for 15 weeks; female A/J mice) treatment significantly reduces the number and size of tumors on the surface of the lungs and reduces the total tumor volume per slide by 64% to 81% compared with the control group[1].

Animal Model: Female A/J mice with vinyl carbamate[1]
Dosage: 30 mg/kg, 60 mg/kg
Administration: Oral administration; daily; for 15 weeks
Result: Significantly reduced the number and size of tumors on the surface of the lungs and reduced the total tumor volume per slide by 64% to 81% compared with the control group.
Clinical Trial
Molecular Weight

352.51

Formula

C₂₄H₃₂O₂

CAS No.

220619-73-8

SMILES

O=C(O)/C=C(C)/C=C/[[email protected]]1[[email protected]](C2=CC=C3C(C)(C)CCC(C)(C)C3=C2)(C)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AGN194204IRX4204NRX194204VTP 194204AGN 194204AGN-194204IRX 4204IRX-4204NRX 194204NRX-194204VTP194204VTP-194204RAR/RXRApoptosisRetinoic acid receptorsRetinoid X receptorsTNF-αlipopolysaccharideIKBαinterleukin-6anti-inflammatoryanticarcinogenicRXRαRXRβRXRγInhibitorinhibitorinhibit

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