NXT629

SKU: orb1708996

Description

NXT629 is a potent and selective PPAR-α antagonist that also inhibits PPARδ, PPARγ, ERβ, GR, and TRβ. It has demonstrated anticancer activity in research, with studies investigating its effects in models of ovarian cancer and melanoma both in vitro and in vivo.

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 1454925-59-7
• MW: 609.78
• Purity: 99.07% (May vary between batches)
• Formula: C₃₅H₃₉N₅O₃S
• SMILES: O=C1N(N=C(N1CC)CCCC=2C=CC(=CC2)C3=NC=C(C=C3)NS(=O)(=O)C=4C=CC=CC4)CC5=CC=C(C=C5)C(C)(C)C
• Target: Thyroid hormone receptor(THR),PPAR,Estrogen/progestogen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.56 mM);DMSO:100 mg/mL (163.99 mM)

Bioactivity

• Target IC50:
  ERβ:15.2 μM|PPARγ (human):15 μM|PPARα (human):77 nM|GR:32.5 μM|PPARδ (human):6 μM
• In Vivo:
  NXT629 exhibits low oral bioavailability in mice and rats. NXT629 administered intraperitoneally (30 mg/kg once daily for 6 weeks) significantly slowed down the growth of subcutaneous SKOV-3 tumors in nude mice and showed inhibition of subcutaneous B16F10 tumor growth in C57Bl/6 mice. In addition, NXT629 (30 mg/kg, intraperitoneal injection) showed weak anti-angiogenic activity in FGF-induced angiogenesis. NXT629 (3 and 30 mg/kg, intraperitoneal injection) also reduced experimental metastasis of B16F10 melanoma cells in the lungs of mice.
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• In Vitro:
  NXT629 (compound 33) is a potent and selective PPAR-α antagonist with an IC50 of 77 nM for human PPARα, as well as weaker effects on other nuclear hormone receptors (e.g., PPARδ, PPARγ, Erβ, GR, and TRβ) with IC50s of 6.0 μM, 15 μM, 15.2 μM, 32.5 μM, and >100 μM, respectively. The competitive inhibitory ability of NXT629 on PPARα, PPARβ/δ and PPARγ was also validated, with corresponding IC50s of 2.3 μM, 35.1 μM and 6.9 μM, respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NXT 629, NXT629, NXT-629, EstrogenReceptor, GR, Estrogen Receptor, ERβ, hPPARα, hPPARγ, hPPARδ, progestogenReceptor, progestogen Receptor

Compound Identifiers

PubChem CID

71721539