LJN452
Tropifexor
CAS: 1383816-29-2
Molecular Formula: C29H25F4N3O5S
LJN452 - Names and Identifiers
LJN452 - Physico-chemical Properties
| Molecular Formula | C29H25F4N3O5S |
| Molar Mass | 603.58 |
| Density | 1.55±0.1 g/cm3(Predicted) |
| Boling Point | 700.0±65.0 °C(Predicted) |
| pKa | 3.84±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | LJN-452 in vitro pharmacological studies is a human FXR agonist, the selectivity of human FXR is more than 30,000 times higher than other nuclear receptors. In primary human hepatocytes, LJN-452 increased the expression levels of BSEP and SHP. |
| In vivo study | Pharmacokinetic studies in rats showed that Tropifexor had a low clearance rate (CL = 9 ml/min/kg) and a long terminal Half-Life (T1/2=3.7 h). tropifexor was formulated as an aqueous microemulsion formulation with an oral bioavailability of 20% in rats. In mice, administered intravenously, Tropifexor has low clearance, small volume of distribution, and a half-life of 2.6 hours. In dogs, after intravenous injection, Tropifexor has a half-life of 7.4 hours and a volume of distribution of 0.46 L/kg. In single and multiple dose experiments, LJN-452 were able to target FXR in intestinal epithelial cells, resulting in a concentration-dependent increase in FGF-19 levels. In ANIT-induced liver injury model, Tropifexor can improve liver transaminases and fibrosis. |
LJN452 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.657 ml | 8.284 ml | 16.568 ml |
| 5 mM | 0.331 ml | 1.657 ml | 3.314 ml |
| 10 mM | 0.166 ml | 0.828 ml | 1.657 ml |
| 5 mM | 0.033 ml | 0.166 ml | 0.331 ml |
Last Update：2024-01-02 23:10:35
LJN452 - Introduction
Tropifexor, full name Cyclic Pyrroloimidazole DNA-alkylating agent 1549, is a DNA alkylating agent. It has the following properties:
1. Chemical properties: Tropifexor is an organic compound with cyclic pyrrole and imidazole groups in its chemical structure. It has a strong affinity for DNA and can be covalently bound to DNA.
2. Use: Tropifexor is often used as an anticancer drug in the field of biomedicine. It can alkylate the DNA of cancer cells by covalent binding with DNA, thus blocking the process of DNA replication and transcription, and achieving the purpose of inhibiting the growth and division of cancer cells.
3. Preparation method: Tropifexor preparation method is more complex, generally involving multi-step organic synthesis reaction. The specific system cannot be made public for reasons such as patent protection.
4. Safety Information: because Tropifexor is a powerful DNA alkylating agent, it has high toxicity. When using or studying Tropifexor, strictly follow laboratory safety regulations and operating procedures, and wear appropriate protective equipment. Avoid skin contact, inhalation or swallowing. If accidental contact occurs, rinse immediately with plenty of water and seek medical attention. For specific toxicity, Hazard and protection requirements, please refer to the relevant chemical safety data form (SDS) or obtain it from the supplier.
1. Chemical properties: Tropifexor is an organic compound with cyclic pyrrole and imidazole groups in its chemical structure. It has a strong affinity for DNA and can be covalently bound to DNA.
2. Use: Tropifexor is often used as an anticancer drug in the field of biomedicine. It can alkylate the DNA of cancer cells by covalent binding with DNA, thus blocking the process of DNA replication and transcription, and achieving the purpose of inhibiting the growth and division of cancer cells.
3. Preparation method: Tropifexor preparation method is more complex, generally involving multi-step organic synthesis reaction. The specific system cannot be made public for reasons such as patent protection.
4. Safety Information: because Tropifexor is a powerful DNA alkylating agent, it has high toxicity. When using or studying Tropifexor, strictly follow laboratory safety regulations and operating procedures, and wear appropriate protective equipment. Avoid skin contact, inhalation or swallowing. If accidental contact occurs, rinse immediately with plenty of water and seek medical attention. For specific toxicity, Hazard and protection requirements, please refer to the relevant chemical safety data form (SDS) or obtain it from the supplier.
Last Update：2024-04-09 21:04:16
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Spot supply
Product Name: Tropifexor Visit Supplier Webpage Request for quotationCAS: 1383816-29-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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