Company Name: |
Riedel-de Haen AG
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Tel: |
800 558-9160 |
Email: |
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Products Intro: |
Purity:98% (HPLC), solid
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Company Name: |
SIGMA-RBI
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Tel: |
800 736 3690 (Orders) |
Email: |
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Products Intro: |
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| A-134974 DIHYDROCHLORIDE HYDRATE Basic information |
Product Name: | A-134974 DIHYDROCHLORIDE HYDRATE | Synonyms: | N7-[(1'R,2'S,3'R,4'S)-2',3'-DIHYDROXY-4'-AMINOCYCLOPENTYL]-4-AMINO-5-IODOPYRROLOPYRIMIDINE DIHYDROCHLORIDE HYDRATE;A-134974 DIHYDROCHLORIDE HYDRATE;N7-[(1′R,2′S,3′R,4′S)-2′,3′-dihydroxy-4′-aminocyclopentyl]-4-amino-5-iodopyrrolopyrimidine dihydrochloride hydrate | CAS: | | MF: | | MW: | 0 | EINECS: | | Product Categories: | | Mol File: | Mol File | |
| A-134974 DIHYDROCHLORIDE HYDRATE Chemical Properties |
form | solid | color | off-white to light tan |
| A-134974 DIHYDROCHLORIDE HYDRATE Usage And Synthesis |
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. |
| A-134974 DIHYDROCHLORIDE HYDRATE Preparation Products And Raw materials |
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