SPA70 (Synonyms: Specific PXR Antagonist 70) |
| カタログ番号GC49281 |
SPA70 は、540 nM (Ki=390 nM) の IC50 を持つ、ヒト プレグナン X 受容体 (hPXR) の強力かつ選択的なアンタゴニストです。 SPA70 は、がん細胞の化学感受性を高めることができます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 931314-31-7
Sample solution is provided at 25 µL, 10mM.
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SPA70 is a pregnane X receptor (PXR) antagonist (IC50 = 0.51 µM).1 It is selective for PXR over 10 additional nuclear receptors at concentrations greater than 5 µM, as well as over a panel of 384 kinases at 10 µM. SPA70 (0.1-10 µM) inhibits PXR activation induced by rifampicin in HEK293 cells expressing the human receptor. It also inhibits rifampicin-induced activity of the PXR target cytochrome P450 (CYP) isoform 3A4 (CYP3A4) in primary human hepatocytes. SPA70 (200 mg/kg) inhibits PXR agonist-induced CYP3A4-mediated metabolism of midazolam and paclitaxel in human PXR transgenic (hPXR-tg) mice.
1.Lin, W., Wang, Y.-M., Chai, S.C., et al.SPA70 is a potent antagonist of human pregnane X receptorNat. Commun.8(1)741(2017)
| Cas No. | 931314-31-7 | SDF | |
| 同義語 | Specific PXR Antagonist 70 | ||
| Canonical SMILES | COC1=CC(N2N=NC(S(C3=CC=C(C(C)(C)C)C=C3)(=O)=O)=C2C)=C(OC)C=C1 | ||
| Formula | C21H25N3O4S | M.Wt | 415.5 |
| 溶解度 | Chloroform: 10 mg/ml | 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 | 2.4067 mL | 12.0337 mL | 24.0674 mL |
| 5 mM | 0.4813 mL | 2.4067 mL | 4.8135 mL |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4067 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 ddH2O, 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: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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