A2846

A-134974 dihydrochloride hydrate

≥98% (HPLC), solid

• Synonyme(s) : N⁷-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
• Formule empirique (notation de Hill): C₁₁H₁₄IN₅O₂ · 2HCl · xH₂O
• Numéro CAS: 1049737-44-1
• Poids moléculaire : 448.09 (anhydrous basis)
• Numéro MDL: MFCD08692561
• Code UNSPSC : 12352200
• ID de substance PubChem : 24890697
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Forme: solid
• Conditions de stockage: desiccated
• Couleur: off-white to light tan
• Solubilité: H₂O: soluble
• Auteur: Abbott
• Chaîne SMILES: 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
• Clé InChI: INMLNTBMPNIKQK-HWZUHWJPSA-N

Description

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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

Informations légales

Sold under license from Abbott Laboratories.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: Eyeshields, Gloves, type N95 (US)