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Tropifexor

Cat. No. M6201
Tropifexor Structure
Synonym:

LJN452

Size Price Availability Quantity
5mg USD 200  USD200 In stock
10mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis.

Product Citations
Customer Product Validations & Biological Datas
Source Liver Int (2021). Figure 4. Tropifexor (Abmole Bioscience)
Method gavage
Cell Lines Guangxi Bama mini-pigs
Concentrations 1.06 μg/kg
Incubation Time a day since 2 d
Results RT-qPCR analysis showed that the mRNA levels of the cholangiocyte markers KRT7, KRT19 and MMP7 were reduced in BDL + TXR piglets compared with BDL piglets. Western blot analysis showed that the expression of CK19 protein was significantly decreased in the liver samples of BDL + TXR compared with that of BDL piglets.
Source Liver Int (2021). Figure 3. Tropifexor (Abmole Bioscience)
Method gavage
Cell Lines Guangxi Bama mini-pigs
Concentrations 1.06 μg/kg
Incubation Time a day since 2 d
Results Consistently, western blot analysis showed that BDL significantly increased the protein levels of α-SMA and collagen I in the liver samples of BDL piglets but not in that of BDL + TXR piglets
Chemical Information
Molecular Weight 603.58
Formula C29H25F4N3O5S
CAS Number 1383816-29-2
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tully DC, et al. J Med Chem. Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

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Keywords: Tropifexor, LJN452 supplier, Farnesoid X Receptor, inhibitors, activators


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