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142880-36-2

142880-36-2 structure
142880-36-2 structure
  • Name: GM 6001
  • Chemical Name: (R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide
  • CAS Number: 142880-36-2
  • Molecular Formula: C20H28N4O4
  • Molecular Weight: 388.461
  • Catalog: Biochemical Inhibitor Proteases MMP inhibitor
  • Create Date: 2018-03-07 08:00:00
  • Modify Date: 2024-01-01 20:47:06
  • Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.
Name (R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide
Synonyms Ilomastat
(2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide
(S-(R*,S*))-N4-Hydroxy-N{1}-(1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl)-2-(2-methylpropyl)butanediamide
GM6001
(2R)-N4-(hydroxy)-N1-((1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl)-2-(2-methylpropyl)butanediamide
Butanediamide, N-hydroxy-N-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)-, (2R)-
(2R)-N-Hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-isobutylsuccinamide
(2R)-N-Hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxo-2-propanyl]-2-isobutylsuccinamide
Galardin
Description Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.
Related Catalog
Target

Ki: 0.4 nM (MMP-1), 0.5 nM (MMP-2), 27 nM (MMP-3), 3.7 nM (MMP-7), 0.1 nM (MMP-8), 0.2 nM (MMP-9), 3.6 nM (MMP-12), 13.4 nM (MMP-14), 0.36 nM (MMP-26)

In Vitro Ilomastat (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]. Ilomastat (0.1 nM-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, and thus inhibits T-cell homing[4].
In Vivo Ilomastat (GM6001) (400 μg/mL) prevents corneal ulceration after severe alkali injury[2]. Ilomastat (GM6001) significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates in rabbit model after stenting[3].
Animal Admin To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or Ilomastat (GM6001) (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. Ilomastat (GM6001) is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals are euthanized at either 1 week or 10 weeks after the second injury. For biochemical studies, iliac artery tissue is removed under general anesthetic, followed by a fatal intracardiac injection of thiopentol. For histomorphometric studies, iliac arteries are perfusion-fixed in 10% buffered formalin for 20 min at a perfusion pressure of 80 mm Hg.
References

[1]. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug 11;31(31):7152-4.

[2]. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31.

[3]. Li C, et al. Arterial repair after stenting and the effects of GM6001, a matrix metalloproteinase inhibitor. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.

[4]. Leppert D, et al. T cell gelatinases mediate basement membrane transmigration in vitro. J Immunol. 1995 May 1;154(9):4379-89.
Density 1.228±0.06 g/cm3
Molecular Formula C20H28N4O4
Molecular Weight 388.461
Exact Mass 388.211060
PSA 123.32000
LogP 0.83
Appearance Off-white solid
Index of Refraction 1.590
Storage condition 2-8°C
Water Solubility Practically insoluble (0.062 g/L) (25 ºC)
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases 22-24/25
RIDADR NONH for all modes of transport
WGK Germany 3
HS Code 29339900

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title: CAS No. 142880-36-2 | Chemsrc address: https://www.chemsrc.com/en/baike/345873.html

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