4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid
- Product Name
- 4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid
- CAS No.
- 1773489-72-7
- Chemical Name
- 4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid
- Synonyms
- CS-2689;LMB-763;EOS-61760;Nidufexor;Nidufexor(LMB-763);(Nidufexor)EOS-61760;Nidufexor, 10 mM in DMSO;inhibit,Inhibitor,Autophagy,NR1H4,FXR,Nidufexor,LMB-763,LMB763,LMB 763;4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid;Benzoic acid, 4-[[[(8-chloro-1,4-dihydro-1-methyl[1]benzopyrano[4,3-c]pyrazol-3-yl)carbonyl](phenylmethyl)amino]methyl]-
- CBNumber
- CB73142726
- Molecular Formula
- C27H22ClN3O4
- Formula Weight
- 487.93
- MOL File
- 1773489-72-7.mol
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid Property
- Boiling point:
- 781.1±60.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: soluble; Ethanol: soluble
- form
- A solid
- pka
- 4.17±0.10(Predicted)
- color
- White to off-white
- InChIKey
- JYTIXGYXBIBOMN-UHFFFAOYSA-N
- SMILES
- C(O)(=O)C1=CC=C(CN(C(C2=NN(C)C3C4=CC(Cl)=CC=C4OCC=32)=O)CC2=CC=CC=C2)C=C1
N-Bromosuccinimide Price
- Product number
- CS-0039398
- Product name
- Nidufexor
- Purity
- 98.96%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0039398
- Product name
- Nidufexor
- Purity
- 98.96%
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0039398
- Product name
- Nidufexor
- Purity
- 98.96%
- Packaging
- 50mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- CS-0039398
- Product name
- Nidufexor
- Purity
- 98.96%
- Packaging
- 100mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- DC21243
- Product name
- Nidufexor(LMB-763)
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1700
- Updated
- 2021/12/16
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid Chemical Properties,Usage,Production
Uses
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH)[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].
| 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]. |
References
[1] Chianelli D, et al. Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880. DOI:10.1021/acs.jmedchem.9b01621
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid Preparation Products And Raw materials
Raw materials
Preparation Products
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid Suppliers
- Tel
- 0595-22008920; 18120708884
- 393612455@qq.com
- Country
- China
- ProdList
- 255
- Advantage
- 58
- Tel
- 020-39119399 18927568969
- Fax
- 020-39119999
- isunpharm@qq.com
- Country
- China
- ProdList
- 4720
- Advantage
- 55
- Tel
- 021-52996696,15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4768
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 984
- Advantage
- 55
- Tel
- 0512-63009836 18994340901
- Fax
- 0512-63006936
- helen@struchem.com
- Country
- China
- ProdList
- 3981
- Advantage
- 60
- Tel
- 13816613772
- Fax
- QQ: 12922499
- huahero21@sina.com
- Country
- China
- ProdList
- 2391
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8000
- Advantage
- 62
- Tel
- Fax
- -
- 13006575422@163.com
- Country
- China
- ProdList
- 6355
- Advantage
- 58
- Tel
- 021-QQ:65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9125
- Advantage
- 58