144928-48-3
Chemical Structure
GP515
- CAS No.: 144928-48-3
- Formula:C10H13BrN6O3
- Molecular Weight:345.15
InChIKey: LTTBFVDMHCIDPM-BHBWVORQSA-N
SMILES: O[C@H]1[C@@H](O)[C@H](N2C3=NC=NC(N)=C3C(Br)=N2)O[C@@H]1CN
Biological Activity: GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock[1][2][3][4].
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GP515 | GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock. | |||||||||||||||||||||
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- [1]. Bulut K, et al. Long-Term Effects of the Adenosine Kinase Inhibitor GP-515 on Hepatic Microcirculation Following Hemorrhagic Shock. Eur J Trauma. 2003;29:139–144.
- [2]. Gu JW, et al. Inhibition of adenosine kinase induces expression of VEGF mRNA and protein in myocardial myoblasts. Am J Physiol Heart Circ Physiol. 2000;279(5):H2116-H2123. [Content Brief]
- [3]. Siegmund B, Rieder F, Albrich S, Wolf K, Bidlingmaier C, Firestein GS, Boyle D, Lehr HA, Loher F, Hartmann G, Endres S, Eigler A. Adenosine kinase inhibitor GP515 improves experimental colitis in mice. J Pharmacol Exp Ther. 2001 Jan;296(1):99-105. [Content Brief]
- [4]. Eigler A, Matschke V, Hartmann G, Erhardt S, Boyle D, Firestein GS, Endres S. Suppression of TNF-alpha production in human mononuclear cells by an adenosine kinase inhibitor. J Leukoc Biol. 2000 Jul;68(1):97-103. [Content Brief]
Keywords
