Synonym
BXT 51072; BXT51072; BXT-51072; ALT-2074; ALT2074; ALT 2074;
IUPAC/Chemical Name
2H-1,2-Benzoselenazine, 3,4-dihydro-4,4-dimethyl-
InChi Key
FXRYWOJYVGJZLE-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H13NSe/c1-10(2)7-11-12-9-6-4-3-5-8(9)10/h3-6,11H,7H2,1-2H3
SMILES Code
CC1(C)CN[Se]C2=CC=CC=C12
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
BXT 51072, also known as ALT-2074, belongs to a class of drugs called "glutathione peroxidase mimics."
In vitro activity:
The two compounds that have the highest GPx activity, BXT-51072 and BXT-51077, were shown to be the most efficient inhibitors of leukocyte recruitment by human umbilical vein endothelial cells (HUVEC), upon incubation with neutrophils (10-fold excess over HUVEC) and with 1 ng/ml TNF-alpha for 1 or 3.5 h.
Reference: Free Radic Biol Med. 1998 Aug;25(3):270-81. https://pubmed.ncbi.nlm.nih.gov/9680172/
In vivo activity:
Administration of an antioxidant (BXT-51072) to Hp 2 mice reduced myocardial injury after IR by more than 80% (p = 0.003), but no myocardial protection was provided by the antioxidant to Hp 1 mice.
Reference: J Am Coll Cardiol. 2007 Jan 2;49(1):82-7. https://pubmed.ncbi.nlm.nih.gov/17207726/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
226.18
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Gosgnach W, Messika-Zeitoun D, Gonzalez W, Philipe M, Michel JB. Shear stress induces iNOS expression in cultured smooth muscle cells: role of oxidative stress. Am J Physiol Cell Physiol. 2000 Dec;279(6):C1880-8. doi: 10.1152/ajpcell.2000.279.6.C1880. PMID: 11078703.
2. Moutet M, d'Alessio P, Malette P, Devaux V, Chaudière J. Glutathione peroxidase mimics prevent TNFalpha- and neutrophil-induced endothelial alterations. Free Radic Biol Med. 1998 Aug;25(3):270-81. doi: 10.1016/s0891-5849(98)00038-0. PMID: 9680172.
3. Blum S, Asaf R, Guetta J, Miller-Lotan R, Asleh R, Kremer R, Levy NS, Berger FG, Aronson D, Fu X, Zhang R, Hazen SL, Levy AP. Haptoglobin genotype determines myocardial infarct size in diabetic mice. J Am Coll Cardiol. 2007 Jan 2;49(1):82-7. doi: 10.1016/j.jacc.2006.08.044. Epub 2006 Dec 13. PMID: 17207726.
4. Castagné V, Clarke PG. Neuroprotective effects of a new glutathione peroxidase mimetic on neurons of the chick embryo's retina. J Neurosci Res. 2000 Feb 15;59(4):497-503. doi: 10.1002/(SICI)1097-4547(20000215)59:4<497::AID-JNR4>3.0.CO;2-B. PMID: 10679788.
In vitro protocol:
1. Gosgnach W, Messika-Zeitoun D, Gonzalez W, Philipe M, Michel JB. Shear stress induces iNOS expression in cultured smooth muscle cells: role of oxidative stress. Am J Physiol Cell Physiol. 2000 Dec;279(6):C1880-8. doi: 10.1152/ajpcell.2000.279.6.C1880. PMID: 11078703.
2. Moutet M, d'Alessio P, Malette P, Devaux V, Chaudière J. Glutathione peroxidase mimics prevent TNFalpha- and neutrophil-induced endothelial alterations. Free Radic Biol Med. 1998 Aug;25(3):270-81. doi: 10.1016/s0891-5849(98)00038-0. PMID: 9680172.
In vivo protocol:
1. Blum S, Asaf R, Guetta J, Miller-Lotan R, Asleh R, Kremer R, Levy NS, Berger FG, Aronson D, Fu X, Zhang R, Hazen SL, Levy AP. Haptoglobin genotype determines myocardial infarct size in diabetic mice. J Am Coll Cardiol. 2007 Jan 2;49(1):82-7. doi: 10.1016/j.jacc.2006.08.044. Epub 2006 Dec 13. PMID: 17207726.
2. Castagné V, Clarke PG. Neuroprotective effects of a new glutathione peroxidase mimetic on neurons of the chick embryo's retina. J Neurosci Res. 2000 Feb 15;59(4):497-503. doi: 10.1002/(SICI)1097-4547(20000215)59:4<497::AID-JNR4>3.0.CO;2-B. PMID: 10679788.
1: Blum S, Asaf R, Guetta J, Miller-Lotan R, Asleh R, Kremer R, Levy NS, Berger FG, Aronson D, Fu X, Zhang R, Hazen SL, Levy AP. Haptoglobin genotype determines myocardial infarct size in diabetic mice. J Am Coll Cardiol. 2007 Jan 2;49(1):82-7. doi: 10.1016/j.jacc.2006.08.044. Epub 2006 Dec 13. PMID: 17207726.
2: Tuvlin JA, Kane SV. Novel therapies in the treatment of ulcerative colitis. Expert Opin Investig Drugs. 2003 Mar;12(3):483-90. doi: 10.1517/13543784.12.3.483. PMID: 12605569.
3: Bayes M, Rabasseda X, Prous JR. Gateways to Clinical Trials. Methods Find Exp Clin Pharmacol. 2002 Apr;24(3):159-84. PMID: 12087878.
4: Gosgnach W, Messika-Zeitoun D, Gonzalez W, Philipe M, Michel JB. Shear stress induces iNOS expression in cultured smooth muscle cells: role of oxidative stress. Am J Physiol Cell Physiol. 2000 Dec;279(6):C1880-8. doi: 10.1152/ajpcell.2000.279.6.C1880. PMID: 11078703.
5: Castagné V, Clarke PG. Neuroprotective effects of a new glutathione peroxidase mimetic on neurons of the chick embryo's retina. J Neurosci Res. 2000 Feb 15;59(4):497-503. doi: 10.1002/(SICI)1097-4547(20000215)59:4<497::AID- JNR4>3.0.CO;2-B. PMID: 10679788.
6: Moutet M, d'Alessio P, Malette P, Devaux V, Chaudière J. Glutathione peroxidase mimics prevent TNFalpha- and neutrophil-induced endothelial alterations. Free Radic Biol Med. 1998 Aug;25(3):270-81. doi: 10.1016/s0891-5849(98)00038-0. PMID: 9680172.
7: d'Alessio P, Moutet M, Coudrier E, Darquenne S, Chaudiere J. ICAM-1 and VCAM-1 expression induced by TNF-alpha are inhibited by a glutathione peroxidase mimic. Free Radic Biol Med. 1998 Apr;24(6):979-87. doi: 10.1016/s0891-5849(97)00396-1. PMID: 9607608.
8: d'Alessio P, Moutet M, Marsac C, Chaudière J. Modulation pharmacologique des altérations du cytosquelette endothélial induites par le péroxyde d'hydrogène et par le TNF-alpha [Pharmacological modulation of alterations of endothelial cytoskeleton induced by hydrogen peroxyde and by TNF-alpha]. C R Seances Soc Biol Fil. 1996;190(2-3):289-97. French. PMID: 8869238.
9: Chaudière J, Moutet M, D'Alessio P. Protection antioxydante et anti- inflammatoire des cellules endothéliales vasculaires par de nouveaux mimes synthétiques de la glutathion peroxydase [Antioxidant and anti-inflammatory protection of vascular endothelial cells by new synthetic mimics of glutathione
