| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A649835-1mg |
1mg |
期货  |
| |
| A649835-5mg |
5mg |
期货 |
|
| 英文别名 | PD119160 | (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 | AGN 194204 | VTP 194204 | SCHEMBL3437269 | (+)-VTP-194204 | AGN 4204 | E98723 | Q27269803 | 2,4-Pentadienoic acid, 3-met |
|---|---|
| 规格或纯度 | ≥99% |
| 英文名称 | AGN194204 |
| 生化机理 | AGN194204 (IRX4204) 是一种口服活性和选择性 RXR 激动剂，对 RXRα 、RXRβ 和 RXRγ 的 K d 值分别为 0.4 nM、3.6 nM 和 3.8 nM，EC 50 s 分别为 0.2 nM、0.8 nM 和 0.08 nM。AGN194204 对 RAR 无活性。AGN194204 对 RAR 不具有活性。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激动剂 |
| 作用机制 | 维甲酸 X 受体激动剂 |
| 产品介绍 |
AGN194204 (IRX4204) is an orally active and selective RXR agonist with K d values 0.4 nM, 3.6 nM and 3.8 nM and EC 50 s 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. 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. AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female A/J mice with vinyl carbamate 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. Form:Solid |
| 纯度 | ≥99% |
| ALogP | 7.3 |
|---|
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC 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 |
| 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 |
| InChi Key | BOOOLEGQBVUTKC-NVQSDHBMSA-N |
| Smiles | CC(=CC(=O)O)C=CC1CC1(C)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C |
| Isomeric 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 |
| 关联CAS | 220619-73-8 |
| PubChem CID | 9863341 |
| MeSH Entry Terms | AGN 194204;AGN-194204;AGN194204;NRX 194204;NRX-194204;NRX194204 |
| 分子量 | 352.51 |
| 分子量 | 352.500 g/mol |
|---|---|
| XLogP3 | 7.300 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 2 |
| 可旋转键计数Rotatable Bond Count | 4 |
| 精确质量Exact Mass | 352.24 Da |
| 单同位素质量Monoisotopic Mass | 352.24 Da |
| 拓扑极表面积Topological Polar Surface Area | 37.300 Ų |
| 重原子数Heavy Atom Count | 26 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 624.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 2 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 2 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 2 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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