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Purity: ≥98%
BGP-15 HCl is a potent and novel PARP inhibitor that can protect against heart failure and atrial fibrillation in mice. At 200 μM, BGP-15 inhibits the oxidative damage caused by imatinib mesylate, reduces the loss of high-energy phosphates, modifies the signaling effect of imatinib mesylate by blocking p38 MAP kinase and JNK activation, and stimulates Akt and GSK-3beta phosphorylation. An in-vivo investigation revealed that in two mouse models of HF and AF, BGP-15 enhanced cardiac function and decreased arrhythmic episodes. BGP-15 was linked to higher IGF1R phosphorylation in these models.
| ln Vitro |
At 200 μM, BGP-15 inhibits the oxidative damage caused by imatinib mesylate, stops the consumption of high-energy phosphates, and modifies the signaling effects of imatinib mesylate by inhibiting p38 MAP damage, JNK activation, and Sensing Akt and GSK-3beta[5].
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| ln Vivo |
In old mdx mice, BGP-15 (15 mg/kg, cervical) had no effect on skeletal muscle pathology [1]. Although it did not stop diaphragm muscle atrophy, 10 days of BGP-15 therapy significantly increased diaphragm muscle fiber function in the stent model (about 100%). Additionally, by preventing myosin PTM linked to PARP-1 suppression and HSP72 activation, this therapy enhances septal content and function [2]. The effects of BGP-15 (15 mg/kg daily in saline) were assessed using morphological, cardiac function, and electrocardiographic measures in independent cohorts of Ntg mice or normal wild-type mice. Treatment with BGP-15 decreased the growth in lung weight and atrial size. Arrhythmias can be prevented or their consequences lessened with BGP-15 medication. In the HF+AF paradigm, BGP-15 processing is linked to the PR interval [3]. In pillow-fed rabbits, BGP-15 (10 and 30 mg/kg) raised polenta by 50% and 70%, respectively, but not in normal rabbits. Following a 5-day course of therapy with BGP-15, the rate of mutation infusion enhanced in hereditary insulin-resistant GK in a dose-dependent way. When compared to carbon dioxide, the most effective dose is 20 mg/kg, which increases insulin load by 71% [4].
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| Animal Protocol |
Male adult HF+AF and Ntg mice, who are approximately 4 months old, are given BGP-15 (15 mg/kg daily in saline) or left untreated (oral gavage with saline or no gavage) for 4 weeks. In the HF+AF model, gavage with saline has no effect on morphological or functional parameters. Thus, mice receiving saline injection and mice left untreated (no gavage) are grouped together and referred to as HF+AF control. ECG and echocardiography scans are carried out both before and after therapy.
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| References |
[1]. Kennedy TL, et al. BGP-15 Improves Aspects of the Dystrophic Pathology in mdx and dko Mice with Differing Efficacies in Heart and Skeletal Muscle. Am J Pathol. 2016 Dec;186(12):3246-3260
[2]. Salah H, et al. The chaperone co-inducer BGP-15 alleviates ventilation-induced diaphragm dysfunction. Sci Transl Med. 2016 Aug 3;8(350):350ra10 [3]. Sapra G, et al. The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice. Nat Commun. 2014 Dec 9;5:5705 [4]. Literati-Nagy B, et al. Improvement of insulin sensitivity by a novel drug candidate, BGP-15, in different animal studies. Metab Syndr Relat Disord. 2014 Mar;12(2):125-31 [5]. Sarszegi Z, et al. 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 [6]. Szabados E, et al. BGP-15, a nicotinic amidoxime derivate protecting heart from ischemia reperfusion injury through modulation of poly(ADP-ribose) polymerase. Biochem Pharmacol. 2000 Apr 15;59(8):937-45 |
| Molecular Formula |
C14H24CL2N4O2
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|---|---|
| Molecular Weight |
351.27
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| Exact Mass |
350.13
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| Elemental Analysis |
C, 47.87; H, 6.89; Cl, 20.19; N, 15.95; O, 9.11
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| CAS # |
66611-37-8
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| Related CAS # |
66611-38-9; 66611-37-8 (HCl)
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| Appearance |
White solid powder
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| SMILES |
C1CCN(CC1)CC(CO/N=C(/C2=CN=CC=C2)\N)O.Cl.Cl
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| InChi Key |
ISGGVCWFTPTHIX-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
N'-(2-hydroxy-3-piperidin-1-ylpropoxy)pyridine-3-carboximidamide;dihydrochloride
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| Synonyms |
BGP15 hydrochloride; BGP15 HCl; BGP15; BGP 15; BGP-15
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~284.68 mM)
DMSO : ~11.33 mg/mL (~32.25 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (284.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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