product name BGP-15
Description: BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice. BGP-15 (200 μM) prevents the imatinib mesylate-induced oxidative damages, attenuates the depletion of high-energy phosphates, alters the signaling effect of imatinib mesylate by preventing p38 MAP kinase and JNK activation, and induced the phosphorylation of Akt and GSK-3beta. In-vivo study indicated that BGP-15 improved cardiac function and reduced arrhythmic episodes in two HF and AF mouse models. In these models, BGP-15 was associated with increased phosphorylation of IGF1R.
References: Am J Pathol. 2016;186:3246-3260; Sci Transl Med. 2016;8(350):350ra103; Nat Commun. 2014;5:5705.
351.27
Formula
C14H24Cl2N4O2
CAS No.
66611-37-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 11.33 mg/mL
Water:
Ethanol:
Solubility (In vivo)
Synonyms
N-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotinimidamide dihydrochloride
other peoduct :
| In Vitro |
In vitro activity: BGP-15 (200 μM) prevents the imatinib mesylate-induced oxidative damages, attenuates the depletion of high-energy phosphates, alters the signaling effect of imatinib mesylate by preventing p38 MAP kinase and JNK activation, and induced the phosphorylation of Akt and GSK-3beta. Kinase Assay: Cell Assay: Previous study showed that BGP-15 at 200 μM could prevent the imatinib-induced oxidative damages, attenuate the depletion of high-energy phosphates, alter the signaling effect of imatinib by preventing p38 MAP kinase and JNK activation, and also induce the Akt and GSK-3β phosphorylation. |
|---|---|
| In Vivo | BGP-15 (15 mg/kg, p.o.) does not improve skeletal muscle pathology in older mdx mice. In a rat model, 10 days of BGP-15 treatment greatly improves diaphragm muscle fiber function (by about 100%), although it does not reverse diaphragm atrophy. The treatment also provides protection from myosin PTMs associated with HSP72 induction and PARP-1 inhibition, resulting in improvement of mitochondrial function and content. BGP-15 (15 mg/kg per day in saline) treatment has no effect in Ntg mice or an independent cohort of normal adult wild-type mice based on morphology, cardiac function and ECG parameters. Treatment with BGP-15 attenuates the increase in atrial size and lung weight. BGP-15 treatment is able to prevent or reduce episodes of arrhythmia. BGP-15 treatment is associated with a reduced PR interval in the HF+AF model. |
| Animal model | |
| Formulation & Dosage | |
| References | Am J Pathol. 2016 Dec;186(12):3246-3260; Sci Transl Med. 2016 Aug 3;8(350):350ra103; Nat Commun. 2014 Dec 9;5:5705. |
