1454925-59-7
1454925-59-7 structure
- Name: NXT629
- Chemical Name: NXT629
- CAS Number: 1454925-59-7
- Molecular Formula: C35H39N5O3S
- Molecular Weight: 609.78
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PPAR
- Create Date: 2019-02-13 17:28:48
- Modify Date: 2024-01-13 19:04:35
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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].
| Name | NXT629 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
hPPARα:77 nM (IC50) hPPARδ:6 μM (IC50) hPPARγ:15 μM (IC50) ERβ:15.2 μM (IC50) GR:32.5 μM (IC50) |
| In Vitro | NXT629 (Compound 33) is a potent, selective 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 also competitively inhibits mousse PPARα, PPARβ/δ and PPARγ, with IC50s of 2.3, 35.1, 6.9 μM, resepctively[2]. |
| 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]. |
| References |
| Molecular Formula | C35H39N5O3S |
|---|---|
| Molecular Weight | 609.78 |
| Storage condition | 2-8℃ |