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BGP-15PARP inhibitor

BGP-15

Catalog No. B6086
Size Price Stock Qty
5mg $129.00 In stock
10mg $225.00 In stock
50mg $959.00 In stock

Tel: +1-832-696-8203

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

BGP-15

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Chemical Properties

Cas No. 66611-37-8 SDF Download SDF
Chemical Name N-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotinimidamide dihydrochloride
Canonical SMILES N=C(NOCC(O)CN1CCCCC1)C2=CN=CC=C2.Cl.Cl
Formula C14H24Cl2N4O2 M.Wt 351.27
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Ki= 57 μM

BGP-15 is a PARP inhibitor.

As a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase(PARP), PARP inhibitors are considered a potential treatment for stroke and myocardial infarction.

In vitro: 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 [1].

In vivo: 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. Moreover, cardiac-specific IGF1R transgenic overexpression in mice recapitulated the protection caused by BGP-15. The authors further demonstrated that BGP-15 with IGF1R could provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70 [2].

Clinical trial: A safety and efficacy of BGP-15 in patients with type 2 diabetes mellitus has been scheduled, however, this study is now terminated due to the funding support withdrawn. (https://clinicaltrials.gov/ct2/show/NCT01069965 term=BGP-15&rank=1)

References:
[1] Sarszegi Z,Bognar E,Gaszner B,Kónyi A,Gallyas F Jr,Sumegi B,Berente Z.  BGP-15, a PARP-inhibitor, prevents imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. Mol Cell Biochem.2012 Jun;365(1-2):129-37.
[2] Sapra G,Tham YK,Cemerlang N,et al.  The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice. Nat Commun.2014 Dec 9;5:5705.