A2846

A-134974 dihydrochloride hydrate

≥98% (HPLC), solid

• 同義詞: N⁷-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
• 經驗公式（希爾表示法）: C₁₁H₁₄IN₅O₂ · 2HCl · xH₂O
• CAS號碼: 1049737-44-1
• 分子量：: 448.09 (anhydrous basis)
• MDL號碼: MFCD08692561
• 分類程式碼代碼: 12352200
• PubChem物質ID: 24890697
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 形狀: solid
• 儲存條件: desiccated
• 顏色: off-white to light tan
• 溶解度: H₂O: soluble
• 起源: Abbott
• SMILES 字串: 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 密鑰: INMLNTBMPNIKQK-HWZUHWJPSA-N

描述

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.

特點和優勢

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

法律資訊

Sold under license from Abbott Laboratories.

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable
• 個人防護裝備: Eyeshields, Gloves, type N95 (US)