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 Estructura química

No. CAS : 1346554-47-9

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  

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Based on 1 publication(s) in Google Scholar

SKI2852 Related Antibodies

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Descripciòn

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.
Peso molecular

543.65

Fòrmula

C27H34FN5O4S
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8394 mL 9.1971 mL 18.3942 mL
5 mM 0.3679 mL 1.8394 mL 3.6788 mL
View the 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 1.25 mg/mL (2.30 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 98.89%

SDS (251 KB)

COA (250 KB)

Instrucciones de manejo (2659 KB)
Referencias

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
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
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SKI2852 Related Classifications

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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Nombre del producto:
SKI2852
Cat. No.:
HY-19325
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SAFETY DATA SHEET (SDS)

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