A2846

A-134974 dihydrochloride hydrate

≥98% (HPLC), solid

• Sinonimo/i: N⁷-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
• Formula empirica (notazione di Hill): C₁₁H₁₄IN₅O₂ · 2HCl · xH₂O
• Numero CAS: 1049737-44-1
• Peso molecolare: 448.09 (anhydrous basis)
• Numero MDL: MFCD08692561
• Codice UNSPSC: 12352200
• ID PubChem: 24890697
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Forma fisica: solid
• Condizioni di stoccaggio: desiccated
• Colore: off-white to light tan
• Solubilità: H₂O: soluble
• Ideatore: Abbott
• Stringa SMILE: 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; INMLNTBMPNIKQK-HWZUHWJPSA-N

Descrizione

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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

Note legali

Sold under license from Abbott Laboratories.

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable
• Dispositivi di protezione individuale: Eyeshields, Gloves, type N95 (US)