A-134974 dihydrochloride hydrate
SIGMA/A2846 - ≥98% (HPLC), solid
Synonym: N7-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate
CAS Number: 1049737-44-1
Empirical Formula (Hill Notation): C11H14IN5O2 · 2HCl · xH2O
Molecular Weight: 448.09 (anhydrous basis)
MDL Number: MFCD08692561
Linear Formula: C11H14IN5O2 · 2HCl · xH2O
Product Type: Chemical
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This image depicts A2846-5MG.
This image depicts A2846-5MG.
| assay | ≥98% (HPLC) |
| color | off-white to light tan |
| form | solid |
| InChI | 1S/C11H14IN5O2.2ClH.H2O/c |
| InChI key | INMLNTBMPNIKQK-HWZUHWJPSA |
| originator | Abbott |
| Quality Level | 100  |
| SMILES string | O.Cl.Cl.N[C@H]1C[C@H]([C@ |
| solubility | H2O: soluble |
| storage condition | desiccated |
| 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. |
| Biochem/physiol Actions: | A-134974 is a novel and selective adenosine kinase inhibitor. In a rat model of neuropathic pain, intraperitoneal A-134974 reduced tactile allodynia and hyperalgesia in a dose-dependent manner (IC50 = 60 pM). |
| Features and Benefits: | This compound was developed by Abbott . To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here . |
| Legal Information: | Sold under license from Abbott Laboratories. |
| Packaging: | 5 mg in glass bottle |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| UNSPSC | 12352200 |