2. Metabolic Enzyme/Protease
  3. ADAMTS
  4. Aldumastat

Aldumastat  (Synonyms: GLPG1972; S201086)

Cat. No.: HY-137430 Purity: 99.54%
SDS COA Handling Instructions

Molarity Calculator

Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC50=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC50=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research.

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

Aldumastat Chemical Structure

Aldumastat Chemical Structure

CAS No. : 1957278-93-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Aldumastat Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC50=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC50=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research[1].

IC50 & Target[1]

ADAMTS-5

19 nM (IC50)

ADAMTS-4

156 nM (IC50)

MMP-2

1158 nM (IC50)

MMP-14

>3198 nM (IC50)

In Vivo

GLPG1972 (oral gavage; 5 mg/kg; single dose) displays a favorable PK profile in mice, rats, and dogs. The oral availability (F%) for mice, rats, and dogs are 25%, 58% and 97%, respectively[1].

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

406.43

Formula

C20H24F2N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CCN1C2=CC(F)=CC(F)=C2)C[C@@H]1C)CC[C@](NC3=O)(C4CC4)C(N3)=O
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 (246.04 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 2.4604 mL 12.3022 mL 24.6045 mL
5 mM 0.4921 mL 2.4604 mL 4.9209 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (12.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (12.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 2.4604 mL 12.3022 mL 24.6045 mL 61.5112 mL
5 mM 0.4921 mL 2.4604 mL 4.9209 mL 12.3022 mL
10 mM 0.2460 mL 1.2302 mL 2.4604 mL 6.1511 mL
15 mM 0.1640 mL 0.8201 mL 1.6403 mL 4.1007 mL
20 mM 0.1230 mL 0.6151 mL 1.2302 mL 3.0756 mL
25 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4604 mL
30 mM 0.0820 mL 0.4101 mL 0.8201 mL 2.0504 mL
40 mM 0.0615 mL 0.3076 mL 0.6151 mL 1.5378 mL
50 mM 0.0492 mL 0.2460 mL 0.4921 mL 1.2302 mL
60 mM 0.0410 mL 0.2050 mL 0.4101 mL 1.0252 mL
80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7689 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6151 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Aldumastat 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:

Aldumastat1957278-93-1GLPG1972 S201086GLPG 1972GLPG-1972S201086S 201086S-201086ADAMTSAdamalysin-like metalloproteinase with thrombospondin motifsdibenzocyclooctadiene lignanalzheimer's diseaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Aldumastat
Cat. No.:
HY-137430
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.