SML2175
GSK360A
≥98% (HPLC)
Sinonimo/i:
GSK 1120360A, GSK1120360A, N-[[1-(2-Cyclopropylethyl)-6-fluoro-1,2-dihydro-4-hydroxy-2-oxo-3-quinolinyl]carbonyl]glycine, N-[[1-(2-Cyclopropylethyl)-6-fluoro-4-hydroxy-2-oxo-1,2-dihydro-3-quinolinyl]carbonyl]glycine
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Informazioni su questo articolo
Formula empirica (notazione di Hill):
C17H17FN2O5
Numero CAS:
Peso molecolare:
348.33
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Prezzi e disponibilità al momento non sono disponibili
Servizio Tecnico
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Permettici di aiutartiassay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
OC(C1=C(N2CCC3CC3)C=CC(F)=C1)=C(C(NCC(O)=O)=O)C2=O
InChI
1S/C17H17FN2O5/c18-10-3-4-12-11(7-10)15(23)14(16(24)19-8-13(21)22)17(25)20(12)6-5-9-1-2-9/h3-4,7,9,23H,1-2,5-6,8H2,(H,19,24)(H,21,22)
InChI key
TYHRZQVUPPODPT-UHFFFAOYSA-N
Biochem/physiol Actions
GSK360A (GSK1120360A) is an orally active HIF-prolyl 4-hydroxylase (HIF-PHD) inhibitor that targets all three HIF-PHD isoforms (PHD1 > PHD2 = PHD3) with high potency (IC50 from 10-120 nM) in a 2-oxoglutarate (2-OG)-competitive manner. GSK360A promotes cardiomyocyte mitochondrial aerobic glycolysis under normoxic conditions by stabilizing cellular hypoxia-inducible factor-1 (HIF-1) and thereby upregulating HIF-1α target genes transcription (50 μM for 8 hrs in murine cardiomyocyte HL-1 cultures), including pyruvate dehydrogenase kinase-1 (PDK1) and hexokinase II (HKII). GSK360A treatment is shown to protect against acute myocardial ischemia–reperfusion injury (IRI) both in cultures and in rats in vivo (30 mg/kg p.o.) by reducing mitochondrial permeability transition pore (MPTP) opening and oxidative stress during IRI.
Orally active, potent HIF prolyl 4-hydroxylase (PHD) inhibitor with in vitro and in vivo efficacy against acute myocardial ischemia-reperfusion injury (IRI).
Classe di stoccaggio
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Weike Bao et al.
Journal of cardiovascular pharmacology, 56(2), 147-155 (2010-08-18)
Hypoxia inducible factors (HIFs) are transcription factors that are regulated by HIF-prolyl 4-hydroxylases (PHDs) in response to changes in oxygen tension. Once activated, HIFs play an important role in angiogenesis, erythropoiesis, proliferation, cell survival, inflammation, and energy metabolism. We hypothesized
Sang-Ging Ong et al.
Cardiovascular research, 104(1), 24-36 (2014-07-30)
Hypoxia-inducible factor-1 (HIF-1) has been reported to promote tolerance against acute myocardial ischaemia-reperfusion injury (IRI). However, the mechanism through which HIF-1 stabilization actually confers this cardioprotection is not clear. We investigated whether HIF-1α stabilization protects the heart against acute IRI
J P Gumucio et al.
Bone & joint research, 6(1), 57-65 (2017-01-22)
Rotator cuff tears are among the most frequent upper extremity injuries. Current treatment strategies do not address the poor quality of the muscle and tendon following chronic rotator cuff tears. Hypoxia-inducible factor-1 alpha (HIF-1α) is a transcription factor that activates