| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
In RAW264.7 macrophages, treatment with AGN194204 (NRX194204; 0-100 nM; 24 hours; E) inhibits the release of nitric oxide and interleukin-6, as well as the degradation of IKBα, caused by lipopolysaccharide and tumor necrosis factor-α. Similar to cells, capacities [1]. Breast cancer cells undergo apoptosis when treated with AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) [1].
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| ln Vivo |
The number and size of lung surface tumors as well as the total tumor volume per slide were considerably reduced by AGN194204 (NRX194204; 30–60 mg/kg; oral; daily; for 15 weeks; female A/J mice) treatment. The reduction was 64%–81% when compared to the control group [1].
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| Cell Assay |
Apoptosis analysis[1]
Cell Types: SK-BR-3 human breast cancer cells Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induction of apoptosis in lung and breast cancer cells. Western Blot Analysis[1] Cell Types: E, RAW Cell Tested Concentrations: 0 nM, 1 nM, 10 nM and 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Ability to block the release of nitric acid induced by lipopolysaccharide and tumor necrosis factor-alpha oxides and interleukin-6 and degradation of IKBα in RAW264.7 macrophage-like cells. |
| Animal Protocol |
Animal/Disease Models: Female A/J mice vinyl carbamate [1]
Doses: 30 mg/kg, 60 mg/kg Route of Administration: oral; daily; for 15 weeks Experimental Results: Compared with the control group, lung surface The number and size of tumors was Dramatically diminished, with the total tumor volume per slide diminished by 64% to 81%. |
| References |
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| Additional Infomation |
Nrx194204 has been used in trials studying the treatment of Parkinson's Disease and Non-small Cell Lung Cancer.
Rexinoid NRX 194204 is an orally bioavailable synthetic retinoid X receptor (RXR) agonist with potential antineoplastic and anti-inflammatory activities. Rexinoid NRX 194204 selectively binds to and activates RXRs. Because RXRs can form heterodimers with several nuclear receptors (NRs), RXR activation by this agent may result in a broad range of gene expression depending on the effector DNA response elements activated. Rexinoid NRX 194204 may inhibit the tumor-necrosis factor (TNF)-mediated release of nitric oxide (NO) and interleukin 6 (IL6) and may inhibit tumor cell proliferation. This agent appears to be less toxic than RAR-selective ligands. |
| Molecular Formula |
C24H32O2
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|---|---|
| Molecular Weight |
352.51
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| Exact Mass |
352.24
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| CAS # |
220619-73-8
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| PubChem CID |
9863341
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| Appearance |
White to off-white solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
624
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C/C(=C\C(=O)O)/C=C/[C@@H]1C[C@]1(C)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C
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| InChi Key |
BOOOLEGQBVUTKC-NVQSDHBMSA-N
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| InChi Code |
InChI=1S/C24H32O2/c1-16(13-21(25)26)7-8-18-15-24(18,6)17-9-10-19-20(14-17)23(4,5)12-11-22(19,2)3/h7-10,13-14,18H,11-12,15H2,1-6H3,(H,25,26)/b8-7+,16-13+/t18-,24-/m1/s1
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| Chemical Name |
(2E,4E)-3-methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid
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| Synonyms |
IRX 4204; IRX-4204; IRX4204
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~35 mg/mL (~99.29 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8368 mL | 14.1840 mL | 28.3680 mL | |
| 5 mM | 0.5674 mL | 2.8368 mL | 5.6736 mL | |
| 10 mM | 0.2837 mL | 1.4184 mL | 2.8368 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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