SPA70
Based on 1 publication(s) in Google Scholar
SPA70 is a potent and selective antagonist of human pregnane X receptor (hPXR), with an IC50 of 540 nM (Ki=390 nM). SPA70 can enhance the chemosensitivity of cancer cells.
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- 純度: 98.0%
- CAS 番号: 931314-31-7
- 分子式: C21H25N3O4S
- 分子量:415.51
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 SPA70
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生物活性
IC50: 540 nM (hPXR)[1]
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Cell Line:A549, A549/TR, H460, H460/TR cells
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Concentration:PA70 (0.001-30 μM) + PTX (0.001-30 μM)
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Incubation Time:72 h
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Result:SPA70 alone showed IC₅₀ values of 2.41 μM (A549) and 5.62 μM (A549/TR), while combination with PTX synergistically reduced cell viability (CI < 1.0) in both sensitive and resistant cells.
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Cell Line:A549/TR
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Concentration:SPA70 (10 μM) + PTX (2 nM)
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Incubation Time:48 h
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Result:Combination treatment increased apoptotic cells to 15.25% (vs. 7.3% in control) via Annexin V/PI staining, accompanied by elevated ROS levels.
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Cell Line:A549/TR
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Concentration:SPA70 (10 μM) + PTX (2 nM)
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Incubation Time:48 h
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Result:Combination treatment induced S-phase arrest (48.6% reduction in EdU incorporation) and mitotic defects (multipolar spindles) compared to controls.
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Cell Line:A549/TR, H460/TR
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Concentration:SPA70 (10 μM) + PTX (2 nM)
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Incubation Time:48 h
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Result:Reduced P-gp, PXR, and Tip60 expression, increased cleaved PARP and phosphorylated MLKL, indicating apoptosis and necroptosis activation.
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Animal Model:hPXR transgenic mice (male, 8–15 weeks, 20–25 g) + rifampicin-induced Cyp3a11 activation model[1]
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Dosage:200 mg/kg (i.p., saline + 7.5% PEG400)
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Administration:i.p. injection, once daily for 3 days
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Result:Reduced rifampicin-induced Cyp3a11 mRNA/protein expression by 70% and prolonged anesthesia duration by 2-fold compared to vehicle controls.
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Animal Model:BALB/c Nude mice (male, 6-8 weeks, 20-22 g) + A549/TR xenograft model[2].
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Dosage:30 mg/kg (i.p., 90% PBS + 5% PEG300 + 5% ethanol)
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Administration:i.p. injection, 3 times/week for 4 weeks
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Result:A549/TR xenograft: SPA70 combined with PTX (5 mg/kg) suppressed tumor growth by 89.5% (TGI), decreased P-gp and PXR expression by 60%, and increased cleaved caspase-3-positive cells by 3-fold.
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Animal Model:hPXR/CYP3A4 humanized mice (male, 8-10 weeks, 20-25 g) + hemorrhagic shock (HS) model[3]
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Dosage:150 mg/kg (i.p., DMSO + cremophor EL)
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Administration:i.p. injection, once daily for 3 days
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Result:Blocked rifampicin-induced CYP3A4 expression, reduced hepatic necrosis (Suzuki score: 2.1 vs. 4.5 in vehicle), and attenuated oxidative stress (4-HNE and 8-OHdG staining).
化学情報
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CAS 番号 931314-31-7
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性状 Solid
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分子量 415.51
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分子式 C21H25N3O4S
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Color Off-white to pink
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SMILES
CC1=C(S(=O)(C2=CC=C(C(C)(C)C)C=C2)=O)N=NN1C3=CC(OC)=CC=C3OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Struct Mol Biol
Cytoplasmic PXR regulates glucose metabolism by binding mRNAs and modulating their stability. [Abstract]2025 Aug 12. PMID: 40797049
溶剤 & 溶解度
DMSO : 40 mg/mL (96.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4067 mL | 12.0334 mL | 24.0668 mL | 60.1670 mL |
| 5 mM | 0.4813 mL | 2.4067 mL | 4.8134 mL | 12.0334 mL | |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4067 mL | 6.0167 mL | |
| 15 mM | 0.1604 mL | 0.8022 mL | 1.6045 mL | 4.0111 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2033 mL | 3.0084 mL | |
| 25 mM | 0.0963 mL | 0.4813 mL | 0.9627 mL | 2.4067 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8022 mL | 2.0056 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5042 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2033 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL |
SPA70 関連分類
HY-124830 関連分類
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