PCSK9-IN-11
Based on 1 publication(s) in Google Scholar
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research.
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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。
- 純度 : 99.30%
- CAS 番号: 2882035-56-3
- 分子式: C16H17ClFN5O3
- 分子量:381.79
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 PCSK9-IN-11
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生物活性
製品説明
IC50 & Target
IC50: 5.7 μM (PCSK9)[1]
体外実験
PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly decreases PCSK9 protein level and increases LDLR expression in a dose dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0, 2.5, 5, 12.5, 25 μM
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Incubation Time:24 h
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Result:Significantly decreased PCSK9 protein level in a dose dependent manner. Markedly increased LDLR expression in a dose dependent manner. Significantly and dose-dependently increased DiI-LDL uptake by around 1.7 folds.
体内実験
PCSK9-IN-11 (30 mg/kg, IG, once a day for 8 weeks) significantly suppresses hepatic PCSK9 expression and slightly reduces serum PCSK9 level[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 mice[1]
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Dosage:0, 250, 500 or 1000 mg/kg
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Administration:Intragastrically administrated, single dose
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Result:Exhibited a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg. Did not affected the body weight, behavioral and survival characteristics of mice.
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Animal Model:ApoE KO mice (under high-fat diet (HFD))[1]
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Dosage:30 mg/kg
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Administration:Intragastric administration, once a day for 8 weeks
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Result:Significantly suppressed hepatic PCSK9 expression and slightly reduced serum PCSK9 level.
化学情報
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CAS 番号 2882035-56-3
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性状 Solid
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分子量 381.79
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分子式 C16H17ClFN5O3
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Color White to off-white
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SMILES
O=C(N1C)N(C)C2=C(N(CC3=CC=CC(Cl)=C3F)C(NCCO)=N2)C1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
NAT10 promotes gallbladder cancer progression by remodeling cholesterol metabolism via PCSK9 mRNA acetylation. [Abstract]2026 Apr 16;12(1):251. PMID: 41991932
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (327.41 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). 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 (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 | 2.6192 mL | 13.0962 mL | 26.1924 mL | 65.4810 mL |
| 5 mM | 0.5238 mL | 2.6192 mL | 5.2385 mL | 13.0962 mL | |
| 10 mM | 0.2619 mL | 1.3096 mL | 2.6192 mL | 6.5481 mL | |
| 15 mM | 0.1746 mL | 0.8731 mL | 1.7462 mL | 4.3654 mL | |
| 20 mM | 0.1310 mL | 0.6548 mL | 1.3096 mL | 3.2741 mL | |
| 25 mM | 0.1048 mL | 0.5238 mL | 1.0477 mL | 2.6192 mL | |
| 30 mM | 0.0873 mL | 0.4365 mL | 0.8731 mL | 2.1827 mL | |
| 40 mM | 0.0655 mL | 0.3274 mL | 0.6548 mL | 1.6370 mL | |
| 50 mM | 0.0524 mL | 0.2619 mL | 0.5238 mL | 1.3096 mL | |
| 60 mM | 0.0437 mL | 0.2183 mL | 0.4365 mL | 1.0914 mL | |
| 80 mM | 0.0327 mL | 0.1637 mL | 0.3274 mL | 0.8185 mL | |
| 100 mM | 0.0262 mL | 0.1310 mL | 0.2619 mL | 0.6548 mL |
PCSK9-IN-11 関連分類
HY-152223 関連分類
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