A-134974 dihydrochloride hydrate,5MG,A2846-5MG,Sigma

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订货号 0BS5672
品牌型号 Sigma A2846-5MG
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最小订货量 1件
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产品介绍 Product Description

Biochem/physiol Actions

A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC50 = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED50= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED50 = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED50= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED50 = 100 nmol, i.c.v.) or intraplantar (ED50 >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED50 values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED50= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.
A-134974 is a novel and selective adenosine kinase inhibitor. In a rat model of neuropathic pain, intraperitoneal A-134974 reduced tactile allodynia and hyperalgesia in a dose-dependent manner (IC50 = 60 pM).


Features and Benefits

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.


Legal Information

Sold under license from Abbott Laboratories.


技术参数 Specifications
Quality Segment100
assay≥98% (HPLC)
formsolid
storage conditiondesiccated
color off-white to light tan
solubilityH2O: soluble
originatorAbbott
SMILES stringO.Cl.Cl.N[C@H]1C[C@H]([C@H](O)[C@@H]1O)n2cc(I)c3c(N)ncnc23
InChI1S/C11H14IN5O2.2ClH.H2O/c12-4-2-17(6-1-5(13)8(18)9(6)19)11-7(4)10(14)15-3-16-11;;;/h2-3,5-6,8-9,18-19H,1,13H2,(H2,14,15,16);2*1H;1H2/t5-,6+,8+,9-;;;/m0.../s1
InChI keyINMLNTBMPNIKQK-HWZUHWJPSA-N
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