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LJN 452

Tropifexor

CAS: 1383816-29-2

Molecular Formula: C29H25F4N3O5S

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LJN 452 - Names and Identifiers

Name Tropifexor
Synonyms LJN452
CS-2712
LJN 452
CPD1549
LJN-452
Tropifexor
LJN452,Tropifexor
Tropifexor (LJN452)
2-[(1R,3r,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylic acid
CAS 1383816-29-2

LJN 452 - Physico-chemical Properties

Molecular FormulaC29H25F4N3O5S
Molar Mass603.58
Density1.55±0.1 g/cm3(Predicted)
Boling Point700.0±65.0 °C(Predicted)
pKa3.84±0.10(Predicted)
Storage Condition-20℃
In vitro studyLJN-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 studyPharmacokinetic 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.

LJN 452 - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.657 ml8.284 ml16.568 ml
5 mM0.331 ml1.657 ml3.314 ml
10 mM0.166 ml0.828 ml1.657 ml
5 mM0.033 ml0.166 ml0.331 ml
Last Update:2024-01-02 23:10:35

LJN 452 - 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.
Last Update:2024-04-09 21:04:16
LJN 452
Supplier List
MedChemExpress (MCE)
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CAS: 1383816-29-2
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SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
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Shanghai Macklin Biochemical Co., Ltd
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Email: Int06@meryer.com
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Shanghai Yuanye Bio-Technology Co., Ltd.
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Product Name: Tropifexor Visit Supplier Webpage Request for quotation
CAS: 1383816-29-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
MedChemExpress (MCE)
Spot supply
Product Name: LJN452 Visit Supplier Webpage Request for quotation
CAS: 1383816-29-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: LJN452 Visit Supplier Webpage Request for quotation
CAS: 1383816-29-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
Shanghai Macklin Biochemical Co., Ltd
Spot supply
Product Name: Tropifexor (LJN452) Visit Supplier Webpage Request for quotation
CAS: 1383816-29-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: Tropifexor Visit Supplier Webpage Request for quotation
CAS: 1383816-29-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
LJN 452
CHEMBRDG-BB 3017966
双胍三辛烷基苯磺酸盐溶液, 1000PPM
2-(2-[(4-METHYLBENZYL)SULFANYL]PHENYL)-5-PHENYL-1,3,4-OXADIAZOLE
金刚烷-1,3-二胺
3,5,7-Triaza-1-azoniatricyclo[3.3.1.13,7]decane, 1-(2-methoxy-2-oxoethyl)-, chloride (1:1)
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