SML1949
Synta66
≥98% (HPLC)
Sinónimos:
4-Pyridinecarboxamide, N-(2′,5′-dimethoxy[1,1′-biphenyl]-4-yl)-3-fluoro-, GSK1349571A, N-(2′,5′-Dimethoxy[1,1′-biphenyl]-4-yl)-3-fluoro-4-pyridinecarboxamide, S66, Synta 66, Synta-66
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Fórmula empírica (notación de Hill):
C20H17FN2O3
Número CAS:
Peso molecular:
352.36
UNSPSC Code:
12352200
NACRES:
NA.77
Servicio técnico
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Permítanos ayudarleQuality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(NC1=CC=C(C2=C(OC)C=CC(OC)=C2)C=C1)C3=CC=NC=C3F
InChI key
GFEIWXNLDKUWIK-UHFFFAOYSA-N
Application
Synta66 has been used:
- as a Ca2+ release-activated calcium (CRAC) channel inhibitor to study its effects on ORAI isoforms
- as an ORAI1 blocker to study its effects on the entry of Ca2+ in chronic lymphocytic leukemia (CLL) B cells
- as a CRAC blocker to study its effects on the influx of Ca2+ by store-operated Ca2+ entry (SOCE) in enamel cells
Biochem/physiol Actions
A selective SOCE inhibitor that blocks CRAC current (ICRAC) without significant off-target potency or affinity.
Synta66 (S66) is a CRAC (Ca2+ release-activated Ca2+) channel inhibitor that blocks SOCE (store-operated Ca2+ entry) upon Ca2+ depletion from intracellular stores by thapsigargin in human vascular smooth muscle cells (VSMCs) with high potency (IC50 = 26 nM & 43 nM based on maximum Ca2+ level & rate of increase, respectly). Synta66 exhibits no affinity toward a range of receptors and ion channels (e.g. L-type Ca2+ channel) and does not affect TRPC1/5-mediated SOCE or store-operated non-selective cationic current. Leukocytes are reported to be less sensitive to CRAC inhibition by Synta66 (IC50 = 1.76 μM/HL-60, 1 ?M/Jurkat, 1.4 μM/rat RBL).
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Antonio Di Sabatino et al.
Journal of immunology (Baltimore, Md. : 1950), 183(5), 3454-3462 (2009-08-04)
Prolonged Ca(2+) entry through Ca(2+) release-activated Ca(2+) (CRAC) channels is crucial in activating the Ca(2+)-sensitive transcription factor NFAT, which is responsible for directing T cell proliferation and cytokine gene expression. To establish whether targeting CRAC might counteract intestinal inflammation, we
Jing Li et al.
British journal of pharmacology, 164(2), 382-393 (2011-05-07)
The aim was to advance the understanding of Orai proteins and identify a specific inhibitor of the associated calcium entry mechanism in vascular smooth muscle cells (VSMCs). Proliferating VSMCs were cultured from human saphenous veins. Intracellular calcium was measured using
Marjolaine Debant et al.
Journal for immunotherapy of cancer, 7(1), 111-111 (2019-04-25)
Dysregulation in calcium (Ca2+) signaling is a hallmark of chronic lymphocytic leukemia (CLL). While the role of the B cell receptor (BCR) Ca2+ pathway has been associated with disease progression, the importance of the newly described constitutive Ca2+ entry (CE)