Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C14H22N4O2 |
| Molecular Weight | 278.3501 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(CONC(=N)C1=CC=CN=C1)CN2CCCCC2
InChI
InChIKey=MVLOQULXIYSERZ-UHFFFAOYSA-N
InChI=1S/C14H22N4O2/c15-14(12-5-4-6-16-9-12)17-20-11-13(19)10-18-7-2-1-3-8-18/h4-6,9,13,19H,1-3,7-8,10-11H2,(H2,15,17)
| Molecular Formula | C14H22N4O2 |
| Molecular Weight | 278.3501 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
N-Gene Research Laboratories is developing BGP-15 (NP-51), a small molecule, orally available, indirect Jun kinase (JNK) inhibitor and insulin sensitiser, for glycaemic control in patients with type-2 diabetes mellitus, and as an adjunct treatment for insulin resistance due to antipsychotics or obesity. In March 2002, N-Gene Research Laboratories granted Allos Therapeutics an exclusive license to its intellectual property surrounding BGP 15 in the US. BGP-15 has previously been used in clinical trials for the treatment of skeletal muscle pathology associated with Type 2 Diabetes (through insulin sensitization), Duchenne Muscular Dystrophy (DMD) and heart failure (through anti-inflammatory and anti-fibrotic mechanisms). Via its action as a modulator of the cytoprotective response to cellularstress, and specifically as a poly (ADP-ribose) polymerase (PARP) inhibitor, heat shock protein-inducer, membrane lipid therapeutic and an antioxidant inducer, BGP-15 has previously been shown to protect against skeletal muscle dysfunction, damage and wasting.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22350755 |
120.0 µM [IC50] |
PubMed
| Title | Date | PubMed |
|---|---|---|
| BGP-15 improves contractile function of regenerating soleus muscle. | 2018-04 |
|
| BGP-15 Protects against Oxaliplatin-Induced Skeletal Myopathy and Mitochondrial Reactive Oxygen Species Production in Mice. | 2017 |
|
| BGP-15 Improves Aspects of the Dystrophic Pathology in mdx and dko Mice with Differing Efficacies in Heart and Skeletal Muscle. | 2016-12 |
|
| BGP-15, a nicotinic amidoxime derivate protecting heart from ischemia reperfusion injury through modulation of poly(ADP-ribose) polymerase. | 2000-04-15 |
Sample Use Guides
The efficacy and safety of BGP-15 were compared with placebo in insulin-resistant patients in a 28-day dose-ranging study. Forty-seven nondiabetic patients with impaired glucose tolerance were randomly assigned to 4 weeks of treatment with 200 or 400 mg of BGP-15 or placebo. BGP-15 at 200 or 400 mg significantly improved insulin sensitivity in insulin-resistant, nondiabetic patients during treatment compared to placebo and was safe and well-tolerated.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10692558
Kinetic analysis showed a mixed-type (noncompetitive) inhibition by BGP-15 of nuclear poly(ADP-ribose) polymerase (PARP) with a K(i) = 57 +/- 6 uM.
| Substance Class |
Chemical
Created
by
admin
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Edited
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Mon Mar 31 22:40:43 GMT 2025
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| Record UNII |
28ENT76V8K
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Validated (UNII)
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