2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. HSD-016

HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research.

For research use only. We do not sell to patients.

HSD-016 Chemical Structure

HSD-016 Chemical Structure

CAS No. : 946396-92-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 418 In-stock
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 620 In-stock
25 mg USD 1250 In-stock
50 mg USD 2000 In-stock
100 mg USD 3200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

HSD-016 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research[1].

IC50 & Target

IC50: 1 nM (mouse 11β-HSD1), 8 nM (rat 11β-HSD1), 11 nM (human 11β-HSD1)[1]
Clinical Trial
Molecular Weight

514.46

Formula

C21H21F7N2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=C(C=CC(F)=C1)N2C[C@@H](C)N(CC2)S(=O)(C3=CC([C@@](O)(C(F)(F)F)C)=CC=C3)=O)(F)F
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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (194.38 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 1.9438 mL 9.7189 mL 19.4379 mL
5 mM 0.3888 mL 1.9438 mL 3.8876 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.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.86 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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 1.9438 mL 9.7189 mL 19.4379 mL 48.5946 mL
5 mM 0.3888 mL 1.9438 mL 3.8876 mL 9.7189 mL
10 mM 0.1944 mL 0.9719 mL 1.9438 mL 4.8595 mL
15 mM 0.1296 mL 0.6479 mL 1.2959 mL 3.2396 mL
20 mM 0.0972 mL 0.4859 mL 0.9719 mL 2.4297 mL
25 mM 0.0778 mL 0.3888 mL 0.7775 mL 1.9438 mL
30 mM 0.0648 mL 0.3240 mL 0.6479 mL 1.6198 mL
40 mM 0.0486 mL 0.2430 mL 0.4859 mL 1.2149 mL
50 mM 0.0389 mL 0.1944 mL 0.3888 mL 0.9719 mL
60 mM 0.0324 mL 0.1620 mL 0.3240 mL 0.8099 mL
80 mM 0.0243 mL 0.1215 mL 0.2430 mL 0.6074 mL
100 mM 0.0194 mL 0.0972 mL 0.1944 mL 0.4859 mL
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HSD-016 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:

HSD-016946396-92-5HSD016HSD 01611β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenasetype 2 diabetesorally activeInhibitorinhibitorinhibit

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