PDSinh-C01
PDSinh-C01 is a reversible, non-competitive pendrin (SLC26A4) inhibitor with an IC50 of 2.5 μM. PDSinh-C01 inhibits pendrin-mediated Cl−/SCN− exchange activity, reduces cell counts, protein levels, and pro-inflammatory cytokine production in bronchoalveolar lavage fluid. PDSinh-C01 can be used in research related to acute lung injury and cystic fibrosis.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2128304-65-2
- 分子式: C20H23N3O2S2
- 分子量:401.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
PDSinh-C01 (1-100 μM; 10 min) inhibits pendrin-mediated Cl−/SCN− exchange activity in CHO-K1 cells expressing human pendrin, with an IC50 of 5.29 μM[1].
PDSinh-C01 (0.1-30 μM; 24 h) reduces the cell viability of HPAEpiC[1].
PDSinh-C01 (20 μM; 25 h) significantly reduces the expression levels of pendrin and phosphorylated IκB in LPS (HY-D1056)-induced HPAEpiC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated HPAEpiC
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Concentration:20 μM
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Incubation Time:1 h (pre-incubation prior to 24 h LPS stimulation)
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Result:Significantly reduced LPS-increased pendrin/β-actin and phospho-IκB/total IκB ratios to levels comparable to vehicle control.
体内実験
PDSinh-C01 (10 mg/kg; i.p.; administered twice) alleviates LPS-induced acute lung injury in male C57BL/6J mice and reduces key inflammatory and injury markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8 weeks old, 20-25 g, intranasal instillation of 10 mg/kg LPS)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose 1 hour prior to LPS exposure
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Result:Significantly reduced LPS-induced increases in BALF total cell counts, protein concentration, and neutrophil counts compared to the LPS-only group.
Significantly reduced lung injury scores, pendrin protein expression, phospho-IκB protein expression, pendrin mRNA levels, and lung tissue levels of pro-inflammatory cytokines IL-1β, MIP-2, IL-6, and TNF-α compared to the LPS-only group.
Showed significantly higher lung injury scores than in the YS-01-treated pre-treatment group.
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Animal Model:C57BL/6J (male, 8 weeks old, 20-25 g, intranasal instillation of 10 mg/kg LPS)[1]
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Dosage:10 mg/kg
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Administration:i.p.; two doses at 6 and 12 hours after LPS exposure
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Result:Significantly reduced LPS-induced increases in BALF total cell counts, protein concentration, neutrophil counts, and macrophage counts compared to the LPS-only group.
Significantly reduced lung injury scores (with scores significantly lower than in the YS-01-treated post-treatment group), pendrin protein expression, phospho-IκB protein expression, pendrin mRNA levels, and lung tissue levels of pro-inflammatory cytokines IL-1β, MIP-2, IL-6, and TNF-α compared to the LPS-only group.
化学情報
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CAS 番号 2128304-65-2
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分子量 401.55
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分子式 C20H23N3O2S2
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SMILES
CC1=NNC(C2=CC(S(NC3C(C=CC=C4)=C4CCC3)(=O)=O)=C(C)S2)=C1C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Choi HK, et al. The comparison of two pendrin inhibitors, YS-01 and PDSinh-C01, in lipopolysaccharide-induced acute lung injury. Scientific reports. 2026 Jun 23. [Content Brief]
[2]. Lipani A, et al. Modulators of anion channels and transporters as alternative therapeutic agents to normalize airway surface liquid in cystic fibrosis. European journal of medicinal chemistry. 2026 Jan 15;302(Pt 2):118325. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)