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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Jin Zhou et al.
PloS one, 12(9), e0184049-e0184049 (2017-09-08)
There is interest in pharmacologic preconditioning for end-organ protection by targeting the HIF system. This can be accomplished by inhibition of prolyl 4-hydroxylase (PHD). GSK360A is an orally active PHD inhibitor that has been previously shown to protect the failing
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