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A-134974 dihydrochloride hydrate
产品别名
A-134974 dihydrochloride hydrate
N7-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C11H14IN5O2 · 2HCl · xH2O |
Molecular weight | 448.09 (anhydrous basis) |
MDL number | MFCD08692561 |
PubChem Substance ID【PubChem化学物质编号】 | 24890697 |
NACRES | NA.77 |
Biochem/physiol Actions【生化/生理作用】 | 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. |
Features and Benefits【特点和优势】 | This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here. |
Legal Information【法律信息】 | Sold under license from Abbott Laboratories. |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | solid |
color【颜色】 | off-white to light tan |
solubility【溶解性】 | H2O: soluble |
originator【创始人】 | Abbott |
SMILES string | O.Cl.Cl.N[C@H]1C[C@H]([C@H](O)[C@@H]1O)n2cc(I)c3c(N)ncnc23 |
InChI | 1S/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 key | INMLNTBMPNIKQK-HWZUHWJPSA-N |
packaging【包装】 | 5 mg in glass bottle |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |
Personal Protective Equipment【个人防护装备】 | Eyeshields, Gloves, type N95 (US) |