Ilomastat (GM6001, Galardin)

Catalog No.S7157

Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.

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USD 250 In stock
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Ilomastat (GM6001, Galardin) Chemical Structure

Ilomastat (GM6001, Galardin) Chemical Structure
Molecular Weight: 388.46

Validation & Quality Control

Cited by 1 publications:

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.
Targets MMP-8 [1] MMP-9 [1] MMP-26 [1] MMP-1 [1]

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IC50 0.1 nM(Ki) 0.2 nM(Ki) 0.36 nM(Ki) 0.4 nM(Ki)
In vitro GM6001 inhibits human skin fibroblast collagenase with Ki of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. [1] GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. [2]
In vivo Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. [3] In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. [4]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

Collagenase assay Collagenase assay uses the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. Km is found to vary between 1.5 and 4 mM.

Animal Study:

[4]

Animal Models Rabbit
Formulation 50 mM HEPES buffer
Dosages 100 mg/kg/day
Administration subcutaneous

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Grobelny D, et al. Biochemistry, 1992, 31(31), 7152-714.

[2] Leppert D, et al. J Immunol,1995, 154(9), 4379-4389.

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Chemical Information

Download Ilomastat (GM6001, Galardin) SDF
Molecular Weight (MW) 388.46
Formula

C20H28N4O4

CAS No. 142880-36-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 78 mg/mL (200.79 mM)
Ethanol 8 mg/mL warming (20.59 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Butanediamide, N4-hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)-, (2R)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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