1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

BGP-15 

Cat. No.: HY-100828 Purity: >98.0%
Data Sheet SDS Handling Instructions

BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice.

For research use only. We do not sell to patients.
BGP-15 Chemical Structure

BGP-15 Chemical Structure

CAS No. : 66611-37-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $160 In-stock
25 mg $350 In-stock
50 mg $550 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice.

In Vitro

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[5].

In Vivo

BGP-15 (15 mg/kg, p.o.) does not improve skeletal muscle pathology in older mdx mice[1]. 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[2]. 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[3]. BGP-15 (10 and 30 mg/kg) increases insulin sensitivity by 50% and 70%, respectively, in cholesterol-fed but not in normal rabbits. After 5 days of treatment with BGP-15, the glucose infusion rate is increased in a dose-dependent manner in genetically insulin-resistant GK rats. The most effective dose is 20 mg/kg, which shows a 71% increase in insulin sensitivity compared to control group[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01069965 N-Gene Research Laboratories, Inc.|Integrium|Msource Medical Development GmbH|Kinexum LLC|Thermo Fisher Scientific|Haupt Pharma Wülfing GmbH|Barc NV Diabetes Mellitus October 2010 Phase 2
NCT01069965 N-Gene Research Laboratories, Inc.|Integrium|Msource Medical Development GmbH|Kinexum LLC|Thermo Fisher Scientific|Haupt Pharma Wülfing GmbH|Barc NV Diabetes Mellitus October 2010 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.8468 mL 14.2341 mL 28.4681 mL
5 mM 0.5694 mL 2.8468 mL 5.6936 mL
10 mM 0.2847 mL 1.4234 mL 2.8468 mL
Animal Administration
[3]

BGP-15 is formulated in saline.

Adult (appr 4 month) male HF+AF and Ntg mice are administered with BGP-15 (15 mg/kg per day in saline) for 4 weeks by oral gavage or remained untreated (oral gavage with saline or no gavage). Gavage with saline has no effect on morphological or functional parameters in the HF+AF model. Therefore, untreated mice (no gavage) and mice administered saline are combined and referred to as HF+AF control. Echocardiography and ECG studies are performed before and after treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

351.27

Formula

C₁₄H₂₄Cl₂N₄O₂

CAS No.

66611-37-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 11.33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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BGP-15
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