1454925-59-7
Chemical Structure
NXT629
- CAS No.: 1454925-59-7
- Formula:C35H39N5O3S
- Molecular Weight:609.78
IUPAC Name: N-(6-(4-(3-(1-(4-(tert-butyl)benzyl)-4-ethyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)propyl)phenyl)pyridin-3-yl)benzenesulfonamide
InChIKey: IRSFLNXJVJKMDT-UHFFFAOYSA-N
SMILES: O=S(C1=CC=CC=C1)(NC2=CC=C(C3=CC=C(CCCC(N4CC)=NN(CC5=CC=C(C(C)(C)C)C=C5)C4=O)C=C3)N=C2)=O
Biological Activity: NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively[1]. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models[2].
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NXT629 | 98.75% | NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models. | ||||||||||||||||||||
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- [1]. Bravo Y, et al. Identification of the first potent, selective and bioavailable PPARα antagonist. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. [Content Brief]
- [2]. Stebbins KJ, et al. In vitro and in vivo pharmacology of NXT629, a novel and selective PPARα antagonist. Eur J Pharmacol. 2017 Aug 15;809:130-140. [Content Brief]
Keywords
