SKI2852
Based on 1 Customer Validation
SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively.
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- Pureté: 98.89%
- CAS No.: 1346554-47-9
- Formule: C27H34FN5O4S
- Masse moléculaire:543.65
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Metabolism/Protease Compound Library
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Anti-diabetic Compound Library
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Orally Active Compound Library
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Anti-Obesity Compound Library
HY-L087
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
IC50: 1.6 nM (mHSD1), 2.9 nM (hHSD1)[1]
SKI2852 inhibits 11β-HSD1 with an IC50 of 4.4 ± 0.5 nM in HEK293 cells stably transfected with human 11β-HSD1 cDNA[1].
The amide carbonyl group of SKI2852 established a central hydrogen bond interaction with the hydroxyl side chain of Ser170, one of the key residues (Ser170, Tyr183, and Lys 187) that define the catalytic triad for 11β-HSD1 activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo PK Data for SKI2852[1]
| species | iva | pob | ||||||
| CL (L/kg/h) | Vss (L/kg) | t1/2 (h) | AUC (μg × h/mL) | Cmax (μg/mL) | tmax (h) | AUC (μg × h/mL) | F (%) | |
| mousec | 0.42 | 1.1 | 1.7 | 2.35 | 2.21 | 1.0 | 11.26 | 96 |
| ratc | 0.93 | 2.1 | 1.8 | 1.12 | 1.02 | 1.3 | 3.39 | 60 |
| dogd | 0.36 | 2.4 | 4.7 | 1.47 | 1.12 | 2.1 | 11.52 | 98 |
a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. b0.5% methylcellulose and 1% Tween80 was used as vehicle. cDosed iv at 1 mg/kg, po at 5mg/kg. dDosed iv at 0.5 mg/kg, po at 4 mg/kg.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ob/ob mice, diet-induced obesity (DIO) model[1]
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Dosage:20 mg/kg
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Administration:Oral, once daily for 25 days
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Result:Efficiently reduced postprandial glucose and/or blood HbA1c levels and suppressed hepatic mRNA levels of gluconeogenic enzymes. Clearly enhanced hepatic and whole-body insulin sensitivities in a hyperinsulinemic-euglycemic clamp experiment in DIO mice.
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Animal Model:C57BL/6 mice, rats and dogs[1]
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Dosage:0.5 or 4 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Showed good pharmacokinetic profiles.
Chemical Information
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CAS No. 1346554-47-9
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Appearance Solid
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Masse moléculaire 543.65
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Formule C27H34FN5O4S
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Color White to off-white
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SMILES
O=C(C1=NC(N2[C@H](C)CN(C3=CC=C(S(=O)(C)=O)C=C3F)CC2)=NC=C1)N[C@@H]4[C@]5([H])C[C@@]6([H])C[C@](C5)(O)C[C@]4([H])C6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (183.94 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. 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 1.25 mg/mL (2.30 mM); Suspended solution; Need ultrasonic
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
[1]. Ryu JH, et al. Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). J Med Chem. 2016 Nov 23;59(22):10176-10189. [Content Brief]
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 |
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| DMSO | 1 mM | 1.8394 mL | 9.1971 mL | 18.3942 mL | 45.9855 mL |
| 5 mM | 0.3679 mL | 1.8394 mL | 3.6788 mL | 9.1971 mL | |
| 10 mM | 0.1839 mL | 0.9197 mL | 1.8394 mL | 4.5985 mL | |
| 15 mM | 0.1226 mL | 0.6131 mL | 1.2263 mL | 3.0657 mL | |
| 20 mM | 0.0920 mL | 0.4599 mL | 0.9197 mL | 2.2993 mL | |
| 25 mM | 0.0736 mL | 0.3679 mL | 0.7358 mL | 1.8394 mL | |
| 30 mM | 0.0613 mL | 0.3066 mL | 0.6131 mL | 1.5328 mL | |
| 40 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1496 mL | |
| 50 mM | 0.0368 mL | 0.1839 mL | 0.3679 mL | 0.9197 mL | |
| 60 mM | 0.0307 mL | 0.1533 mL | 0.3066 mL | 0.7664 mL | |
| 80 mM | 0.0230 mL | 0.1150 mL | 0.2299 mL | 0.5748 mL | |
| 100 mM | 0.0184 mL | 0.0920 mL | 0.1839 mL | 0.4599 mL |
SKI2852 Related Classifications
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