BGP-15

Investigational

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

Structure Search

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

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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	( + / - )

Description
Sources: https://adisinsight.springer.com/drugs/800013049 | https://www.ncbi.nlm.nih.gov/pubmed/28443020 | https://drugprofiles.informa.com/drug_profiles/2716-bgp-15

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
Poly (ADP-ribose) polymerase 2 Target ID: Poly (ADP-ribose) polymerase Sources: https://www.ncbi.nlm.nih.gov/pubmed/11931842	Inhibitor 8297
Poly [ADP-ribose] polymerase-1 23 Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22350755	Inhibitor 8297		120.0 µM [IC50]

PubMed

Title	Date	PubMed
BGP-15 Protects against Oxaliplatin-Induced Skeletal Myopathy and Mitochondrial Reactive Oxygen Species Production in Mice.	2017	28443020
BGP-15 improves contractile function of regenerating soleus muscle.	2018 Apr	29948663

Sample Use Guides

In Vivo Use Guide

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

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` on `Sat Dec 16 09:27:31 GMT 2023` Edited by `admin` on `Sat Dec 16 09:27:31 GMT 2023`
Record UNII	RLN2GTG4YS
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BGP-15

Common Name

English

R,S-O-(3-PIPERIDINO-2-HYDROXY-1-PROPYL)-NICOTINIC ACID AMIDOXIME DIHYDROCHLORIDE

Common Name

English

3-PYRIDINECARBOXIMIDAMIDE, N-(2-HYDROXY-3-(1-PIPERIDINYL)PROPOXY)-, HYDROCHLORIDE (1:2)

Systematic Name

English

3-PYRIDINECARBOXIMIDAMIDE, N-(2-HYDROXY-3-(1-PIPERIDINYL)PROPOXY)-, DIHYDROCHLORIDE

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

769720