1. Cell Cycle/DNA Damage
  2. PPAR

NXT629 

Cat. No.: HY-114263 Purity: 99.05%
Handling Instructions

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.

For research use only. We do not sell to patients.

NXT629 Chemical Structure

NXT629 Chemical Structure

CAS No. : 1454925-59-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 872 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

IC50 & Target[1][2]

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].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (204.99 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

References
Molecular Weight

609.78

Formula

C₃₅H₃₉N₅O₃S

CAS No.

1454925-59-7

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

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NXT629
Cat. No.:
HY-114263
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NXT629

Cat. No.: HY-114263