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INO-1001

Cat. No. M1785
INO-1001 Structure
Synonym:

3-Aminobenzamide

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in Water USD 40  USD50 In stock
200mg USD 40  USD50 In stock
500mg USD 72  USD90 In stock
1g USD 112  USD140 In stock
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Quality Control
Biological Activity

INO-1001 is a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. The present study tested INO-1001 for its in vivo effect on the chemoresponse of two p53 deficient tumors, human breast cancer MDA-MB-231 and murine mammary carcinoma MCa-K. Doxorubicin was used as the DNA damaging agent and tumor growth delay assay was used as the endpoint. Results showed that INO-1001 was highly effective in enhancing the anti-tumor effects of Doxorubicin for both MDA-MB-231 (EF=1.88) and MCa-K (EF=1.64).

Product Citations
Customer Product Validations & Biological Datas
Source Exp Gerontol (2007). Figure 2. INO-1001
Method i.p.
Cell Lines male Lewis rats
Concentrations 5 mg/kg
Incubation Time 2 h
Results Single dose treatment with the potent PARP-inhibitor INO-1001 notably decreased PAR formation both in the myocardium and the aortic wall.
Protocol
Cell Experiment
Cell lines cultured podocytes
Preparation method Apoptosis detection. Apoptotic nuclei of cultured podocytes were detected on paraformaldehyde-fixed cells using DAPI (4′,6-diamidino-2-phenylindole) staining (1 μg/ml) for 10 min. Cells were analyzed under a fluorescence microscope and assessed for chromatin condensation and segregation. Caspase-3 activity was measured in podocyte extracts using EnzCheck Caspase-3 Assay kit (Molecular Probes) following the manufacturer’s protocol. Nuclear extracts were prepared using Transfactor DB Nuclear extraction kit (Clontech BD Bioscience) following the manufacturer’s protocol. Western blotting was performed using NFκB p50 (Santa Cruz Biotechnology) antibody. NFκB p50 nuclear binding assay was performed using TransFactor Colorimetric kit (Clontech BD) according to the manufacturer’s protocol.
Concentrations 200 nmol/l
Incubation time 45 min
Animal Experiment
Animal models diabetic nephropathy of Leprdb/db mice model
Formulation sterile water
Dosages 60 mg/kg initiated at 5 weeks of age to around 8 weeks of age
Administration oral in drinking water
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 136.15
Formula C7H8N2O
CAS Number 3544-24-9
Purity 99.89%
Solubility DMSO 22 mg/mL
Water ≥ 4 mg/mL
Storage at -20°C
References

[1] Roesner JP, et al. Shock. Therapeutic injection of PARP inhibitor INO-1001 preserves cardiac function in porcine myocardial ischemia and reperfusion without reducing infarct size.

[2] Bedikian AY, et al. Cancer Invest. A phase IB trial of intravenous INO-1001 plus oral temozolomide in subjects with unresectable stage-III or IV melanoma.

[3] Morrow DA, et al. J Thromb Thrombolysis. A randomized, placebo-controlled trial to evaluate the tolerability, safety, pharmacokinetics, and pharmacodynamics of a potent inhibitor of poly(ADP-ribose) polymerase (INO-1001) in patients with ST-elevation myocardial infarction undergoing primary percutaneous coronary intervention: results of the TIMI 37 trial.

[4] Robert S B Clark, et al. J Neurotrauma. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improves water maze performance after traumatic brain injury in mice

[5] Mason KA, et al. Invest New Drugs. INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase, enhances tumor response to doxorubicin.

[6] Radovits T, et al. Exp Gerontol. Single dose treatment with PARP-inhibitor INO-1001 improves aging-associated cardiac and vascular dysfunction.

[7] Csaba Szabo, et al. Diabetes. Poly(ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice

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Keywords: INO-1001, 3-Aminobenzamide supplier, PARP, inhibitors

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