2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. BI-135585

BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research.

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BI-135585

BI-135585 Estructura química

No. CAS : 1114561-85-1

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1 mg Obtener un presupuesto 2 - 3 weeks 1 - 2 weeks 3 - 4 weeks 2 - 3 weeks
5 mg Obtener un presupuesto 2 - 3 weeks 1 - 2 weeks 3 - 4 weeks 2 - 3 weeks
10 mg Obtener un presupuesto 2 - 3 weeks 1 - 2 weeks 3 - 4 weeks 2 - 3 weeks
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  
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Other Forms of BI-135585:

BI-135585 Related Antibodies

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Descripciòn

BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research[1][2].

IC50 & Target

IC50: 13 nM (11β-HSD1)[1]
In Vitro

BI-135585 binds in the substrate binding pocket of the active site of 11β-HSD1. Cellular activity of BI-135585 is examined by determining inhibition of 11β-HSD1 activity in human preadipocytes, the average IC50 is 1 nM[1].
In human adipose tissue ex vivo, BI-135585 inhibits the conversion of cortisone to cortisol with an average IC50 of 11 nM[1].
Abdominal subcutaneous and perirenal adipose tissue was harvested from one, male cynomolgus monkey. BI-135585 (20 hours) reduces enzyme activity in a dose-dependent manner with an IC50 of ~10 nM in perirenal adipose tissue and an IC50 of ~100 nM in abdominal subcutaneous adipose tissue[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BI-135585 Related Antibodies
In Vivo

BI-135585 (compound 11j; 1-3 mg/kg; po) inhibits 67% and 90% of enzyme activity respectively in perirenal adipose tissue in cynomolgus monkey[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

460.56

Fòrmula

C28H32N2O4
No. CAS
SMILES

CC(C)(O)C[C@@]1(C2=CC=CC=C2)OC(N(CC1)[C@H](C3=CC=C(C4=CC(N(C=C4)C)=O)C=C3)C)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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BI-135585 Related Classifications

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

BI-1355851114561-85-1BI135585BI 13558511β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenase11β-HSD1cortisolcortisonediabetesoralInhibitorinhibitorinhibit

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Nombre del producto:
BI-135585
Cat. No.:
HY-105286
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