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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.89%
- CAS. Nr.: 1346554-47-9
- Formel: C27H34FN5O4S
- Molecular Weight:543.65
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-diabetic Compound Library
HY-L040
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Orally Active Compound Library
HY-L061
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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
Biologische Aktivität
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. Nr. 1346554-47-9
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Appearance Solid
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Molecular Weight 543.65
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
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)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 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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