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AZD-9056 hydrochloride
CAS No. 345303-91-5
AZD-9056 hydrochloride( —— )
Catalog No. M14179 CAS No. 345303-91-5
A potent, selective, orally bioavailable P2X7 receptor antagonist; inhibits release of pro-inflammatory mediators from isolated human peripheral monocytes (IL-1β and IL-18) and human alveolar macrophages (IL-1β) with IC50 values of 10-13 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 50 | Get Quote |
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| 5MG | 84 | Get Quote |
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| 10MG | 142 | Get Quote |
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| 25MG | 317 | Get Quote |
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| 50MG | 528 | Get Quote |
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| 100MG | 755 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameAZD-9056 hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, orally bioavailable P2X7 receptor antagonist; inhibits release of pro-inflammatory mediators from isolated human peripheral monocytes (IL-1β and IL-18) and human alveolar macrophages (IL-1β) with IC50 values of 10-13 nM.
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DescriptionA potent, selective, orally bioavailable P2X7 receptor antagonist; inhibits release of pro-inflammatory mediators from isolated human peripheral monocytes (IL-1β and IL-18) and human alveolar macrophages (IL-1β) with IC50 values of 10-13 nM; displays >100-fold selectivity and specificity other P2X receptors; also is an inhibitor of BCRP and weakly inhibited BCRP-mediated transport of methotrexate (IC50=92 uM); significantly reduces disease severity in the streptococcal cell wall (SCW) model of arthritis.Rheumatoid Arthritis Phase 2 Clinical.
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In VitroThe antagonist AZD9056 blocks P2X7 receptors with an IC50 of 11.2 nM in HEK-hP2X7 cell line, indicating a high selectivity of the antagonist for the P2X7 receptor. The P2X7-receptor antagonist AZD9056 has a clear inhibitory effect (IC50=1-3 μM) in mouse microglia BV2 cells. AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC50=92 μM).
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In VivoTreatment with AZD9056 exerts pain-relieving and anti-inflammatory effects. The upregulated expression of interleukin (IL)-1β, IL-6, tumor necrosis factor-α (TNF-α), matrix metalloproteinase-13 (MMP-13), substance P (SP) and prostaglandin E2 (PGE2) which is induced by MIA in cartilage tissues is reversed by AZD9056.
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Synonyms——
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PathwayMembrane Transporter/Ion Channel
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TargetP2X Receptor
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RecptorP2X Receptor
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Research AreaInflammation/Immunology
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IndicationRheumatoid Arthritis
Chemical Information
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CAS Number345303-91-5
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Formula Weight455.46084
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Molecular FormulaC24H36Cl2N2O2
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 34 mg/mL
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SMILESC1C2CC3CC1CC(C2)(C3)CNC(=O)C4=C(C=CC(=C4)CCCNCCCO)Cl.Cl
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Chemical NameBenzamide, 2-chloro-5-[3-[(3-hydroxypropyl)amino]propyl]-N-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-, hydrochloride (1:1)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Hu H, et al. Int J Mol Med. 2016 Dec;38(6):1922-1932.
2. Seeland S, et al. Int J Mol Med. 2016 Dec;38(6):1922-1932.
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