[CAS NO. 1454925-59-7] NXT629
PRODUCTS SPECIFICATIONS [1454925-59-7]
DESCRIPTION [1454925-59-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 609.78 |
| Molecular Formula | C35H39N5O3S |
| 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 |
3 Publications Citing Use of MCE
Summary
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC 50 of 77 nM for human PPARα , shows high selectivity over other nuclear hormone receptor, such as PPARδ , PPARγ , ERβ , GR and TRβ, IC 50 s 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] .
IC50 & Target
|
hPPARα 77 nM (IC 50 ) |
hPPARδ 6 μM (IC 50 ) |
hPPARγ 15 μM (IC 50 ) |
ERβ 15.2 μM (IC 50 ) |
GR 32.5 μM (IC 50 ) |
In Vitro
NXT629 (Compound 33) is a potent, selective PPAR-α antagonist, with an IC 50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, Erβ, GR and TRβ, IC 50 s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively [1] . NXT629 also competitively inhibits mousse PPARα, PPARβ/δ and PPARγ, with IC 50 s of 2.3, 35.1, 6.9 μM, resepctively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NXT629 (Compound 33; 30 mg/kg, i.p.) exhibits good pharmacokinetics in mouse, and significantly decreases Fgf21 (Fibroblast growth factor 21), a PPARα target gene in fasted mice
[1]
.
NXT629 has poor oral bioavailability in mice and rats. NXT629 (30 mg/kg, i.p., daily for 6 weeks) delays growth of subcutaneous SKOV-3 tumors in nude mice, inhibits growth of subcutaneous B16F10 tumors in C57Bl/6 mice. NXT629 (30 mg/kg, i.p.) is weakly anti-angiogenic against FGF-induced angiogenesis. NXT629 (3, 30 mg/kg, i.p.) inhibits experimental metastasis of B16F10 melanoma cells to the mouse lung
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 204.99 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6399 mL | 8.1997 mL | 16.3994 mL |
| 5 mM | 0.3280 mL | 1.6399 mL | 3.2799 mL |
| 10 mM | 0.1640 mL | 0.8200 mL | 1.6399 mL |
References
- [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.
- [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.
