A2846

A-134974 dihydrochloride hydrate

≥98% (HPLC), solid

• Synonym(e): N⁷-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
• Empirische Formel (Hill-System): C₁₁H₁₄IN₅O₂ · 2HCl · xH₂O
• CAS-Nummer: 1049737-44-1
• Molekulargewicht: 448.09 (anhydrous basis)
• MDL-Nummer: MFCD08692561
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 24890697
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: solid
• Lagerbedingungen: desiccated
• Farbe: off-white to light tan
• Löslichkeit: H₂O: soluble
• Ersteller: 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
• InChIKey: INMLNTBMPNIKQK-HWZUHWJPSA-N

Beschreibung

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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

Rechtliche Hinweise

Sold under license from Abbott Laboratories.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• Persönliche Schutzausrüstung: Eyeshields, Gloves, type N95 (US)