Nidufexor
Based on 1 Customer Validation
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
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- Purity: 99.41%
- CAS No.: 1773489-72-7
- 화학식: C27H22ClN3O4
- 분자량:487.93
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
FXR[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | EC50 |
>80 μM
Compound: 1; LMB763
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Agonist activity at human GPBAR1 expressed in Jurkat cells assessed as increase in intracellular cAMP level incubated for 1 hr by fluorescence based assay
Agonist activity at human GPBAR1 expressed in Jurkat cells assessed as increase in intracellular cAMP level incubated for 1 hr by fluorescence based assay
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[PMID: 31940200] |
? 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Han-Wistar rats[1]
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Dosage:0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral gavage, once daily for 14 days
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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].
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1773489-72-7
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Appearance Solid
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분자량 487.93
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화학식 C27H22ClN3O4
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Color White to off-white
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SMILES
CN1C(C2=CC(Cl)=CC=C2OC3)=C3C(C(N(CC4=CC=CC=C4)CC5=CC=C(C(O)=O)C=C5)=O)=N1
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Synonyms
LMB763
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 83.33 mg/mL (170.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0495 mL | 10.2474 mL | 20.4947 mL | 51.2369 mL |
| 5 mM | 0.4099 mL | 2.0495 mL | 4.0989 mL | 10.2474 mL | |
| 10 mM | 0.2049 mL | 1.0247 mL | 2.0495 mL | 5.1237 mL | |
| 15 mM | 0.1366 mL | 0.6832 mL | 1.3663 mL | 3.4158 mL | |
| 20 mM | 0.1025 mL | 0.5124 mL | 1.0247 mL | 2.5618 mL | |
| 25 mM | 0.0820 mL | 0.4099 mL | 0.8198 mL | 2.0495 mL | |
| 30 mM | 0.0683 mL | 0.3416 mL | 0.6832 mL | 1.7079 mL | |
| 40 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.2809 mL | |
| 50 mM | 0.0410 mL | 0.2049 mL | 0.4099 mL | 1.0247 mL | |
| 60 mM | 0.0342 mL | 0.1708 mL | 0.3416 mL | 0.8539 mL | |
| 80 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6405 mL | |
| 100 mM | 0.0205 mL | 0.1025 mL | 0.2049 mL | 0.5124 mL |
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