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5mg |
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25mg |
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Purity: ≥98%
ISO-1, formerly known as MIF Antagonist and ISO-1 and Macrophage Migration Inhibitory Factor, is a MIF inhibitor. ISO-1 has CAS#478336-92-4. INVIVO-6924 Protects Photoreceptors and Reduces Gliosis in Experimental Retinal Detachment. Systemic administration of the MIF inhibitor ISO-1 significantly blocked photoreceptor apoptosis, outer nuclear layer (ONL) thinning, and retinal gliosis. ISO-1 and MIF knockout (MIFKO) had greater accumulation of Müller glia pERK expression in the detached retina, suggesting that Müller survival pathways might underlie the neuroprotective response.
ln Vitro |
Without recombinant MIF added, ISO-1 (0.1–20 μM; 16 hours) has a mild inhibitory effect on Cox-2 secretion [1].
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ln Vivo |
ISO-1 (ip; 3.5–35 mg/kg; twice daily; 2 weeks) has anti-inflammatory properties and increases survival from lethal endotoxemia [2]. Intraperitoneal injection ISO-1 (35 mg/kg, twice daily, 3 days) significantly lowers Flk1 expression in the implants and decreases mean implant size [3].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW 264.7 macrophages Tested Concentrations: 0.1μM, 1μM, 10μM, 20μM Incubation Duration: 16 hrs (hours) Experimental Results: Inhibition of Cox-2 secretion. |
Animal Protocol |
Animal/Disease Models: C57Bl/6 MIF+/+ and MIF–/– mice [2]
Doses: 3.5-35 mg/kg Route of Administration: intraperitoneal (ip) injection; 3.5-35 mg/kg; twice (two times) daily; 2 weeks Experimental Results: Yes Preventing fatal sepsis. Animal/Disease Models: Female C57BL/6-Tg(ACTB-EGFP)1Osb/J mice [3] Doses: 35 mg/kg Route of Administration: intraperitoneal (ip) injection; 35 mg/kg; twice (two times) daily; 3 days Experimental Results: In utero The average size of the endometriotic implants diminished. |
References |
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Additional Infomation |
5-Isoxazoleacetic acid, 4,5-dihydro-3-(4-hydroxyphenyl)-, methyl ester is a member of phenols.
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Molecular Formula |
C12H13NO4
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Molecular Weight |
235.239
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Exact Mass |
235.084
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CAS # |
478336-92-4
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Related CAS # |
478336-92-4;
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PubChem CID |
4633677
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Appearance |
White to off-white solid powder
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Density |
1.3±0.1 g/cm3
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Boiling Point |
365.0±48.0 °C at 760 mmHg
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Melting Point |
114 °C
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Flash Point |
174.6±29.6 °C
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Vapour Pressure |
0.0±0.8 mmHg at 25°C
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Index of Refraction |
1.582
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LogP |
0.89
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
4
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Heavy Atom Count |
17
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Complexity |
308
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Defined Atom Stereocenter Count |
0
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InChi Key |
AIXMJTYHQHQJLU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C12H13NO4/c1-16-12(15)7-10-6-11(13-17-10)8-2-4-9(14)5-3-8/h2-5,10,14H,6-7H2,1H3
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Chemical Name |
4,5-dihydro-3-(4-hydroxyphenyl)-5-isoxazoleacetic acid, methyl ester
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Synonyms |
ISO-1 ISO 1 ISO1 MIF Antagonist Macrophage Migration Inhibitory Factor
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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 |
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) |
DMSO : ~50 mg/mL (~212.55 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (21.25 mM) in 5% DMSO + 95% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 (10.63 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.63 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. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.2510 mL | 21.2549 mL | 42.5098 mL | |
5 mM | 0.8502 mL | 4.2510 mL | 8.5020 mL | |
10 mM | 0.4251 mL | 2.1255 mL | 4.2510 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02284919 | ACTIVE, NOT RECRUITING | Drug: [18F]ISO-1 | Breast Cancer Breast Neoplasm |
University of Pennsylvania | 2014-11 | Phase 1 |
NCT00968656 | COMPLETED | Radiation: PET/CT Other: Laboratory Testing Other: Safety Testing |
Breast Cancer Diffuse Large B-cell Lymphoma Head and Neck Cancer |
Washington University School of Medicine | 2009-01 | Phase 1 |
NCT02204202 | TERMINATED | Drug: [18F]FDG Drug: [18F]ISO-1 |
Lung Disease | Washington University School of Medicine | 2014-02 | |
NCT03057743 | TERMINATED | Device: Positron emission tomography (PET/CT) imaging Device: radiotracer [18F]ISO-1 |
METASTATIC BREAST CANCER | Abramson Cancer Center at Penn Medicine | 2016-04-05 | |
NCT04831892 | COMPLETED | Other: Moisturizer Containing Isosorbide Diesters and Colloidal Oatmeal Other: Moisturizer containing Colloidal Oatmeal only |
Atopic Dermatitis | Integrative Skin Science and Research | 2021-04-12 | Not Applicable |
The MIF inhibitor, ISO-1 reduces endometriotic implant mass. Endometriosis was induced and mice were subsequently treated as described in Materials and Methods. Average endometriotic implant size (mm3) was calculated between treatment groups. Data are displayed as the mean ± SD and are representative of 10 mice per treatment group (N=10). Data was analyzed by unpaired t-tests. Significance was set at p < 0.05 for all comparisons. Asterisks (*) indicates statistical significantly different means. Broken line indicates size of implants at start of experiment (1 mm3).[3]. Nothnick WB, et al. Inhibition of macrophage migration inhibitory factor reduces endometriotic implant size in mice with experimentally induced disease. J Endometr. 2011 Sep 30;3(3):135-142. td> |
ISO-1 induced endometriotic implant regression is associated with reduced expression of the VEGF receptor, Flk1. Endometriosis was induced and mice were subsequently treated as described in Materials and Methods. Endometriotic implants were harvested after measurement and prepared for RNA isolation. Flk1 transcript levels were quantitated as described in Materials and Methods by qRT-PCR and normalized to 18S rRNA levels. Data are displayed as the mean ± SD and are representative of 6 independent samples per time point per treatment (N=6). Data was analyzed by unpaired t-tests. Significance was set at p < 0.05 for all comparisons. Asterisks (*) indicates statistical significantly different means.[3]. Nothnick WB, et al. Inhibition of macrophage migration inhibitory factor reduces endometriotic implant size in mice with experimentally induced disease. J Endometr. 2011 Sep 30;3(3):135-142. td> |
ISO-1 induced regression of endometriotic implant mass is associated with reduced peritoneal fluid MIF activity. Peritoneal fluid was obtained from mice treated with vehicle or ISO-1and MIF activity was determined as described under Materials and Methods. Data are displayed as the mean ± SD and are representative of 9 independent samples per time point per treatment (N=9). Data was analyzed by unpaired t-tests. Significance was set at p < 0.05 for all comparisons. Asterisks (*) indicates statistical significantly different means. One sample was lost during the aspiration process.[3]. Nothnick WB, et al. Inhibition of macrophage migration inhibitory factor reduces endometriotic implant size in mice with experimentally induced disease. J Endometr. 2011 Sep 30;3(3):135-142. td> |