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Purity: =98.40%
Ilomastat (GM-6001; GM6001; Galardin) potent, synthetic, and broad spectrum matrix metalloprotease (MMP) inhibitor that is highly active and belongs to the hydroxamic acid class of reversible metallopeptidase inhibitors with significant biological activity. With Ki values of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, and 0.36 nM, respectively, it inhibits MMP-1/23/7/8/9/12/14/26. Using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5, ilomastat inhibits human skin fibroblast collagenase with a Ki of 0.4 nM. After moderate alkali injury, a combination of aprotinin, fibronectin, fibromastat, and epidermal growth factor promoted stable regeneration of corneal epithelium. Topical application of ilomastat prevented corneal ulceration after severe alkali injury.
| Targets |
Fibroblast collagenase (Ki = 0.4 nM); MMP-1 (IC50 = 1.5 nM); MMP-2 (IC50 = 1.1 nM); MMP-3 (IC50 = 1.9 nM); MMP-9 (IC50 = 0.5 nM ); Thermolysin (Ki = 20 nM); Eastase (Ki = 20 nM)
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| ln Vitro |
Ilomastat (GM6001) inhibits the fibroblast collagenase, thermolysin, and elastase found in human skin, with corresponding Kis values of 0.4 nM, 20 nM, and 20 nM[1]. T-cell-produced gelatinase A and B are inhibited by ilomastat (0.1–10 nM). T-cell homing is inhibited by ilomastat[4].
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| ln Vivo |
Ilomastat (GM6001) (400 μg/mL) orneal ulceration following severe alkali injury in animals[2]. Intimal hyperplasia and intimal collagen content are markedly suppressed by ilomastat (GM6001). After stenting, ilomastat increases the lumen area of arteries but has no effect on the rates of proliferation in a rab
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| Enzyme Assay |
For the collagenase assay, Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt, a synthetic thiol ester substrate, is used at pH 6.5. One to two nanometers of collagenase and one to seven micrometers of substrate are present. A range of 1.5 to 4 mM is found for Km.
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| Cell Assay |
After being exposed to triapine for 72 hours and receiving 20 µM ilomastat concurrently, the viability of the cells was evaluated.
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| Animal Protocol |
Animal Model 1:[4]
Rabbit Doses: 100 mg/kg/day Route of administration: subcutaneous (SC) injection Animal Model 2:[6] Mice Doses: 150 mg/kg/day Formulation: Ilomastat suspension solution was prepared by dissolving in Tween-80, PEG4000, absolute ethanol and distilled water. Route of administration: injected intraperitoneally (IP) once either with 150 mg/kg Ilomastat or vehicle control 2 h before γ-ray radiation. |
| References |
| Molecular Formula |
C20H28N4O4
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| Molecular Weight |
388.46
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| Exact Mass |
388.21
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| Elemental Analysis |
C, 61.84; H, 7.27; N, 14.42; O, 16.47
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| CAS # |
142880-36-2
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| Related CAS # |
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| Appearance |
Beige to brown solid powder
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| SMILES |
CC(C)C[C@H](CC(=O)NO)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)NC
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| InChi Key |
NITYDPDXAAFEIT-DYVFJYSZSA-N
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| InChi Code |
InChI=1S/C20H28N4O4/c1-12(2)8-13(10-18(25)24-28)19(26)23-17(20(27)21-3)9-14-11-22-16-7-5-4-6-15(14)16/h4-7,11-13,17,22,28H,8-10H2,1-3H3,(H,21,27)(H,23,26)(H,24,25)/t13-,17+/m1/s1
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| Chemical Name |
(2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide
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| Synonyms |
Ilomastat; galardin; GM-6001; GM 6001; GM6001
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: [1] ~11mg/mL (28.3 mM) in 2% DMSO + 40% PEG 300 + 2% Tween 80 + ddH2O [2] ~3.3 mg/ml (8.7 mM) in 5% DMSO + 95% coil oil [3] ~27.5mg/ml (70.8 mM) in 5% DMSO + 40% PEG300 + 5% Tween 80: 50% ddH2O Solubility in Formulation 6: 10 mg/mL (25.74 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5743 mL | 12.8713 mL | 25.7427 mL | |
| 5 mM | 0.5149 mL | 2.5743 mL | 5.1485 mL | |
| 10 mM | 0.2574 mL | 1.2871 mL | 2.5743 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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