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品質等級
化驗
≥98% (HPLC)
形狀
solid
顏色
off-white
溶解度
DMSO: soluble >10 mg/mL
儲存溫度
room temp
SMILES 字串
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
InChI 密鑰
ZACJDWOPQROWIK-UHFFFAOYSA-N
基因資訊
human ... ADORA1(134) , ADORA2A(135) , ADORA2B(136) , ADORA3(140)
rat ... Adora1(29290) , Adora2a(25369) , Adora2b(29316)
應用
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
生化／生理作用
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.
特點和優勢
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.
法律資訊
Manufactured and sold under license from Adenosine Therapeutics LLC.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
其他客户在看
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
[3H] MRS 1754, a selective antagonist radioligand for A2B adenosine receptors
Ji XD, et al.
Biochemical Pharmacology, 61(6), 657-663 (2001)
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
Zhan-Guo Gao et al.
iScience, 26(7), 107178-107178 (2023-07-05)
Protein kinase C (PKC) isoforms regulate many important signaling pathways. Here, we report that PKC activation by phorbol 12-myristate 13-acetate (PMA) enhanced A2B adenosine receptor (AR)-mediated, but not β2-adrenergic receptor-mediated, cAMP accumulation, in H9C2 cardiomyocyte-like and HEK293 cells. In addition
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