2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. SKI2852

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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SKI2852

SKI2852 Chemical Structure

CAS No. : 1346554-47-9

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SKI2852 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 1.6 nM (mHSD1), 2.9 nM (hHSD1)[1]
In Vitro

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.

SKI2852 Related Antibodies
In Vivo

SKI2852 (20 mg/kg; oral; once daily for 25 days) significantly reduces blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice[1].
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.

Animal Model: ob/ob mice, diet-induced obesity (DIO) model[1]
Dosage: 20 mg/kg
Administration: Oral, once daily for 25 days
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.
Animal Model: C57BL/6 mice, rats and dogs[1]
Dosage: 0.5 or 4 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic profiles.
Molecular Weight

543.65

Formula

C27H34FN5O4S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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SKI2852 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKI28521346554-47-9SKI 2852SKI-285211β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenaseHEK293HbA1cdiet-induced obesityDIOdiabetesInhibitorinhibitorinhibit

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