A-134974 dihydrochloride hydrate

• 产品号: A2846
• 分子式: C11H18Cl2IN5O3
• 分子量: 466.10279
• 纯 度: ≥98% (HPLC)

产品别名

• 标题: A-134974 dihydrochloride hydrate
• IUPAC标准名: (1S,2R,3S,5R)-3-amino-5-{4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentane-1,2-diol hydrate dihydrochloride
• IUPAC传统名: (1S,2R,3S,5R)-3-amino-5-{4-amino-5-iodopyrrolo[2,3-d]pyrimidin-7-yl}cyclopentane-1,2-diol hydrate dihydrochloride
• 别名: N7-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate

产品登记号

• PubChem SID: 24890697
• MDL号: MFCD08692561

产品性质

• Empirical Formula (Hill Notation): C11H14IN5O2 · 2HCl · xH2O
• 纯度: ≥98% (HPLC)
• 外观: off-white to light tan solid
• 溶解度: H2O: soluble
• 个人保护装置: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• 德国WGK号: 3

产品详细信息

详细说明 (English)

Legal Information
Sold under license from Abbott Laboratories.
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.††

详细说明 (简体中文)

Legal Information
Sold under license from Abbott Laboratories.
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.††