1. Metabolic Enzyme/Protease
  2. MMP
  3. Aldumastat

Aldumastat (Synonyms: GLPG1972; S201086)

Cat. No.: HY-137430
Handling Instructions

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

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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].

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

Molecular Weight

406.43

Formula

C₂₀H₂₄F₂N₄O₃

CAS No.
SMILES

O=C(N(CCN1C2=CC(F)=CC(F)=C2)C[[email protected]@H]1C)CC[[email protected]](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)

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
10 mM 0.2460 mL 1.2302 mL 2.4604 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

AldumastatGLPG1972 S201086GLPG 1972GLPG-1972S201086S 201086S-201086MMPMatrix metalloproteinasesdibenzocyclooctadiene lignanalzheimer's diseaseInhibitorinhibitorinhibit

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Aldumastat
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HY-137430
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