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BI-135585
🥰Excellent
Catalog No. T26794Cas No. 1114561-85-1
Alias BI135585, BI 135585
BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes.
BI-135585
🥰Excellent
Purity: 99.66%
Catalog No. T26794Alias BI135585, BI 135585Cas No. 1114561-85-1
BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $290 | In Stock | |
| 5 mg | $650 | In Stock | |
| 10 mg | $980 | In Stock | |
| 25 mg | $1,670 | In Stock | |
| 50 mg | $2,180 | In Stock |
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Purity:99.66%
ee:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes. |
| Targets&IC50 | the enzyme activity in abdominal subcutaneous adipose tissue (cynomolgus monkey):100 nM, the enzyme activity in perirenal adipose tissue (cynomolgus monkey):10 nM, 11β-HSD1:1 nM, conversion of corticosterone to cortisol:11 nM |
| In vitro | BI-135585 interacts with the substrate binding pocket of the 11β-HSD1 active site. In human preadipocytes, its inhibition of 11β-HSD1 activity was evaluated and found to have an average IC50 of 1 nM. In isolated human adipose tissue, BI-135585 blocked the conversion of corticosterone to cortisol at an average IC50 of 11 nM. [1] A study of abdominal subcutaneous and perirenal adipose tissue from a male cynomolgus monkey showed that BI-135585 (20 hours of action) exhibited dose-dependent inhibition of the enzyme activity in perirenal adipose tissue with an IC50 of approximately 10 nM, while in abdominal subcutaneous adipose tissue the IC50 was approximately 100 nM.[1] |
| In vivo | BI-135585 (compound 11j; 1-3 mg/kg; orally) inhibited the enzyme activity in perirenal adipose tissue of cynomolgus monkeys by 67% and 90%, respectively. [2] |
| Alias | BI135585, BI 135585 |
| Molecular Weight | 460.57 |
| Formula | C28H32N2O4 |
| Cas No. | 1114561-85-1 |
| Smiles | C(C(C)(C)O)[C@]1(OC(=O)N([C@@H](C)C2=CC=C(C=C2)C3=CC(=O)N(C)C=C3)CC1)C4=CC=CC=C4 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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