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Nidufexor, formerly known as LMB 763, is a novel, potent and orally bioactive farnesoid X receptor (FXR) agonist. Nidufexor has the potential for treating of nonalcoholic steatohepatitis (NASH).
| ln Vivo |
Nidufexor (LMB763), in a mouse model of non-alcoholic steatosis (NASH), is a strong and circumferential in vivo FXR gene modulator that decreases fibrosis, inflammation, and steatosis [1]. Partitioning time (t1/2) following moderate Cmax values (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and powder formulations (3, 10, 30, 100, and 300 mg/kg) in structures (aged roughly 10 weeks); 3.9 5.7 6.3 5.6 6.3 h) [1] Nidufexor exhibits distinct half-lives (attention 4.5, adsorption 4.4 and dog 6.8 hours) in animal models following topical studies (attention 3.0, adsorption 5.0 and dog 0.5 mg/kg): Han-Wistar rats[1].
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| Animal Protocol |
Animal/Disease Models: Han-Wistar rats[1]
Doses: 0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (pharmacokinetic/PK/PK Analysis) Route of Administration: po (oral gavage), one time/day for 14 days Experimental Results: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]. |
| References | |
| Additional Infomation |
Nidufexor is under investigation in clinical trial NCT03804879 (Safety, Tolerability and Efficacy of LMB763 in Patients With Diabetic Nephropathy).
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| Molecular Formula |
C27H22CLN3O4
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|---|---|
| Molecular Weight |
487.94
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| Exact Mass |
487.129
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| CAS # |
1773489-72-7
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| Related CAS # |
1773489-72-7;
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| PubChem CID |
118063735
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
781.1±60.0 °C at 760 mmHg
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| Flash Point |
426.2±32.9 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
3.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
755
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JYTIXGYXBIBOMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H22ClN3O4/c1-30-25-21-13-20(28)11-12-23(21)35-16-22(25)24(29-30)26(32)31(14-17-5-3-2-4-6-17)15-18-7-9-19(10-8-18)27(33)34/h2-13H,14-16H2,1H3,(H,33,34)
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| Chemical Name |
4-[(N-benzyl-8-chloro-1-methyl-1,4-dihydro[1]benzopyrano[4,3-c]pyrazole-3-carboxamido)methyl]benzoic acid
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| Synonyms |
LMB 763 LMB-763 LMB763
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~170.78 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0494 mL | 10.2472 mL | 20.4943 mL | |
| 5 mM | 0.4099 mL | 2.0494 mL | 4.0989 mL | |
| 10 mM | 0.2049 mL | 1.0247 mL | 2.0494 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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