SML3561
VCP746
≥98% (HPLC)
别名:
4-(5-Amino-4-benzoyl-3-(3-(trifluoromethyl)phenyl)thiophen-2-yl)-N-(6-(9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ylamino)hexyl)benzamide, N-[6-[[4-[5-Amino-4-benzoyl-3-[3-(trifluoromethyl)phenyl]-2-thienyl]benzoyl]amino]hexyl]adenosine, VCP 746, VCP-746
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所有图片(1)
About This Item
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(C1=CC=C(C=C1)C2=C(C(C(C3=CC=CC=C3)=O)=C(S2)N)C4=CC=CC(C(F)(F)F)=C4)NCCCCCCNC5=C6N=CN(C6=NC=N5)[C@@H]7O[C@@H]([C@H]([C@H]7O)O)CO
生化/生理作用
VCP746 is an adenosine receptor A1 (A1AR) agonist composed of adenosine linked to the A1AR positive allosteric modulator VCP171, allowing greatly improved affinity (KI = 58.9 nM vs. 2.95 μM/adenosine & 1.55 μM/VCP171) and potency (GTPγS binding induction EC50 = 0.89 nM vs. 93.3 nM/adenosine & 977 nM/VCP171; hA1AR-CHO membrane) via bitopic receptor engagement with both orthosteric and allosteric sites, as well as biased agonism toward inhibition of forskolin-stimulated cAMP over ERK1/2 phosphorylation (hA1AR-CHO) without hA3AR agonist potency. VCP746 protects against ischemia/hypoxia-induced death of rat neonatal ventricular cardiomyocytes (1 μM) and embryonic cardiomyoblasts (300 nM) without affecting isolated rat atrial heart rate.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist
Valant C, May LT, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A
Proceedings of the National Academy of Sciences of the USA, 111, 4614-4619 (2014)
Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery
Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT
Biochemical Pharmacology, 99, 101-112 (2016)
Chung H Chuo et al.
Clinical and experimental pharmacology & physiology, 43(10), 976-982 (2016-07-06)
VCP746 is a novel A1 adenosine receptor (A1 AR) biased agonist previously shown to be cytoprotective with no effect on heart rate. The aim of this study was to investigate the potential anti-hypertrophic effect of VCP746 in neonatal rat cardiac
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