NXT629 |
رقم الكتالوجGC32933
One-Click Copy Product Info
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NXT629 هو مضاد PPAR-α قوي وانتقائي وتنافسي ، مع IC50 من 77 نانومتر لـ PPARα البشري ، ويظهر انتقائية عالية على مستقبلات الهرمونات النووية الأخرى ، مثل PPARδ ، PPARγ ، ERβ ، GR و TRβ ، IC50s هي 6.0 ، 15 و 15.2 و 32.5 و> 100 ميكرومتر على التواليNXT629 له نشاط قوي مضاد للورم ويمنع ورم خبيث تجريبي للخلايا السرطانية في النماذج الحيوانية
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1454925-59-7
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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].
[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.
| Cas No. | 1454925-59-7 | SDF | |
| Canonical 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 | ||
| Formula | C35H39N5O3S | M.Wt | 609.78 |
| الذوبان | DMSO : 125 mg/mL (204.99 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6399 mL | 8.1997 mL | 16.3994 mL |
| 5 mM | 328 μL | 1.6399 mL | 3.2799 mL |
| 10 mM | 164 μL | 820 μL | 1.6399 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)