M6316
MRS 1754 hydrate
≥98% (HPLC), solid
别名:
8-[4-[((4-Cyanophenyl)carbamoylmethyl)oxy]phenyl]-1,3-di(n-propyl)xanthine hydrate
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关于此项目
经验公式（希尔记法）:
C26H26N6O4 · xH2O
化学文摘社编号:
分子量:
486.52 (anhydrous basis)
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
MDL number:
产品名称
MRS 1754 hydrate, ≥98% (HPLC), solid
InChI key
ZACJDWOPQROWIK-UHFFFAOYSA-N
SMILES string
O.CCCN1C(=O)N(CCC)c2[nH]c(nc2C1=O)-c3ccc(OCC(=O)Nc4ccc(cc4)C#N)cc3
InChI
1S/C26H26N6O4.H2O/c1-3-13-31-24-22(25(34)32(14-4-2)26(31)35)29-23(30-24)18-7-11-20(12-8-18)36-16-21(33)28-19-9-5-17(15-27)6-10-19;/h5-12H,3-4,13-14,16H2,1-2H3,(H,28,33)(H,29,30);1H2
assay
≥98% (HPLC)
form
solid
color
off-white
solubility
DMSO: soluble >10 mg/mL
storage temp.
room temp
Quality Level
Gene Information
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
Application
MRS 1754 hydrate has been used as an adenosine receptor A2B (RA2B) antagonist:
- to study its effects on endothelial nitric oxide synthase (eNOS) phosphorylation induced by short-term acetate stimulation in human umbilical vein endothelial cells (HUVECs)
- blastema formation in zebrafish
- to serve as a positive control in the anti-sickling assay and to study the role of RA2B in the same
Biochem/physiol Actions
MRS 1754 hydrate is a p-cyanoanilide xanthine derivative. It might act as a potential anti-asthmatic drug.
MRS 1754 hydrate is a potent A2B adenosine receptor antagonist.
Features and Benefits
This compound is featured on the Adenosine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Legal Information
Manufactured and sold under license from Adenosine Therapeutics LLC.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Odailson Santos Paz et al.
European journal of medicinal chemistry, 136, 487-496 (2017-05-22)
Adenosine receptors are considered as potential targets for drug development against several diseases. The discovery of subtype 2B adenosine receptors role in erythrocyte sickling process proved its importance to neglected diseases such as sickle cell anemia, which affects approximately 29.000
Christine Rampon et al.
Purinergic signalling, 10(4), 595-602 (2014-08-03)
A major issue in regenerative medicine is the control of progenitor cell mobilisation. Apoptosis has been reported as playing a role in cell plasticity, and it has been recently shown that apoptosis is necessary for organ and appendage regeneration. In
Vinegar intake enhances flow-mediated vasodilatation via upregulation of endothelial nitric oxide synthase activity
Sakakibara S, et al.
Bioscience, Biotechnology, and Biochemistry, 74(5), 1055-1061 (2010)
X Ji et al.
Biochemical pharmacology, 61(6), 657-663 (2001-03-27)
MRS 1754 [N-(4-cyanophenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)-phenoxy]acetamide] is a selective antagonist ligand of A(2B) adenosine receptors. This is the least well-defined adenosine receptor subtype, and A(2B) antagonists have potential as antiasthmatic drugs. For use as a radioligand, MRS 1754, a p-cyanoanilide xanthine derivative, was
Vikas Saxena et al.
Cell reports, 39(3), 110727-110727 (2022-04-21)
Regulatory T cell (Treg) lymphatic migration is required for resolving inflammation and prolonging allograft survival. Focusing on Treg interactions with lymphatic endothelial cells (LECs), we dissect mechanisms and functional consequences of Treg transendothelial migration (TEM). Using three genetic mouse models of
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