1. Metabolic Enzyme/Protease
    Autophagy
  2. FXR
    Autophagy
  3. Nidufexor

Nidufexor (Synonyms: LMB763)

Cat. No.: HY-109096 Purity: 98.96%
Handling Instructions

Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).

For research use only. We do not sell to patients.

Nidufexor Chemical Structure

Nidufexor Chemical Structure

CAS No. : 1773489-72-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH)[1].

IC50 & Target

FXR[1]

In Vivo

Nidufexor (LMB763) is a potent and specific FXR-gene modulator in vivo, reducing steatosis, inflammation and fibrosis in nonalcoholic steatohepatitis (NASH) murine models[1].
Nidufexor exhibits moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9 5.7 6.3 5.6 6.3 h) following oral administration (3 ,10 ,30, 100, and 300mg/kg) in adult male Wistar Han rats (age approximately 10 weeks)[1]
Nidufexor exhibits terminal elimination half-lives (mouse 4.5, rat 4.4 and, dog 6.8 h) following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg)[1].
Nidufexor exhibits terminal elimination half-lives (mouse 3.5, rat 2.7 and, dog 10.1 h) following oral administration (mouse 10, rat 10 and, dog 2 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Han-Wistar rats[1]
Dosage: 0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage, once daily for 14 days
Result: On day 1 and 13, serum exposure increased approximately dose-proportionally from 0.1 to 100 mg/kg. Exposure at 0.1 and 0.3 mg/kg was likely underestimated on day 13. No significant accumulation was observed[1].
Clinical Trial
Molecular Weight

487.93

Formula

C₂₇H₂₂ClN₃O₄

CAS No.

1773489-72-7

SMILES

CN1C(C2=CC(Cl)=CC=C2OC3)=C3C(C(N(CC4=CC=CC=C4)CC5=CC=C(C(O)=O)C=C5)=O)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (170.78 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0495 mL 10.2474 mL 20.4947 mL
5 mM 0.4099 mL 2.0495 mL 4.0989 mL
10 mM 0.2049 mL 1.0247 mL 2.0495 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NidufexorLMB763LMB 763LMB-763FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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Nidufexor
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