Details
Stereochemistry | RACEMIC |
Molecular Formula | C14H22N4O2.2ClH |
Molecular Weight | 351.272 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.OC(CONC(=N)C1=CC=CN=C1)CN2CCCCC2
InChI
InChIKey=ISGGVCWFTPTHIX-UHFFFAOYSA-N
InChI=1S/C14H22N4O2.2ClH/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);2*1H
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: Poly (ADP-ribose) polymerase Sources: https://www.ncbi.nlm.nih.gov/pubmed/11931842 |
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Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22350755 |
120.0 µM [IC50] |
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.
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FDA ORPHAN DRUG |
769720
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EU-Orphan Drug |
EU/3/13/1122
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admin on Sat Dec 16 09:27:31 GMT 2023 , Edited by admin on Sat Dec 16 09:27:31 GMT 2023
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FDA ORPHAN DRUG |
386512
Created by
admin on Sat Dec 16 09:27:31 GMT 2023 , Edited by admin on Sat Dec 16 09:27:31 GMT 2023
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300000013629
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66611-37-8
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RLN2GTG4YS
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9884807
Created by
admin on Sat Dec 16 09:27:31 GMT 2023 , Edited by admin on Sat Dec 16 09:27:31 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD