Antibodies
INO-1001
- 貨號 Cat. No.
- S1132
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
INO-1001
Catalog No.S1132
INO-1001 is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | INO-1001 is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2. | |||||
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| Targets | PARP | |||||
| IC50 | 50 nM [1] | |||||
| In vitro | INO-1001 (>1 μM) leads to more than 95% inhibition of PARP activity without significant cellular toxicity. In addition, INO-1001 significantly sensitizes CHO cells by blocking most of the DNA repair occurring between radiation fractions. [1] Inhibition of PARP activity by INO-1001 significantly improves endothelial function by enhancing the acetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400 μM H2O2. [2] | |||||
| In vivo | In a db/db (Leprdb/db) mouse model, INO-1001 ameliorates diabetes-induced albumin excretion and mesangial expansion, and also decreases diabetes-induced podocyte depletion. [3] Treatment with INO-1001 (1.6 mg/kg via intracerebral injection) prevents NAD+ depletion and improves water maze performance after controlled cortical impact (CCI) in mice. [4] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| PARP enzyme activity | PARP activity is measured with a PARP Activity Assay Kit. This method measures relative PARP activity by determining the level of incorporation of 3H-NAD into trichloroacetic acid (TCA) precipitable material in the presence of sheared genomic DNA, which activates PARP. The reaction mixture is added directly to washed cultures in 12-well culture plates and the reaction is allowed to proceed for 60 minutes at 37 °C before the cells are removed mechanically, transferred to a microcentrifuge tube, and precipitated with ice-cold 5% TC |
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Animal Study: [3]
| Animal Models | Male db/db (Leprdb/db) mice. |
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| Dosages | ≤60 mg/kg |
| Administration | Administered via p.o. |
| Solubility | 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00271765 | Completed | Acute Myocardial Infarction | Inotek Pharmaceuticals Corporation | 2004-01 | Phase 2 |
| NCT00271167 | Active, not recruiting | Heart Diseases|Postoperative Complications | Inotek Pharmaceuticals Corporation | 2005-10 | Phase 2 |
| NCT00272415 | Terminated | Melanoma | Genentech | 2005-10 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 136.15 |
|---|---|
| Formula | C7H8N2O |
| CAS No. | 3544-24-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 27 mg/mL (198 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 27 mg/mL (198 mM) | ||
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W, | 30 mg/mL | |
| * <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 | 3-aminobenzamide |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.13615 | 1.3615 | 2.723 | 4.0845 |
