AZD-4818

• CAS: 1003566-93-5
• Catalog Number: ACM1003566935
• Category: Antagonists
• Molecular Weight: 567.46
• Molecular Formula: C27H32Cl2N2O7
• Description: AZD-4818 is a chemokine CCR1 antagonist that is used for the treatment of chronic obstructive pulmonary disease.
• Synonyms: AZD-4818; AZD 4818; AZD4818
• IUPAC Name: (S)-2-(2-chloro-5-(3-(5-chloro-3H-spiro[benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropoxy)-4-(methylcarbamoyl)phenoxy)-
• Canonical SMILES: CC(C)(OC1=CC(OC[C@@H](O)CN2CCC3(CC2)OC4=CC=C(Cl)C=C4C3)=C(C(NC)=O)C=C1Cl)C(O)=O
• InChI: InChI=1S/C27H32Cl2N2O7/c1-26(2,25(34)35)37-23-12-22(19(11-20(23)29)24(33)30-3)36-15-18(32)14-31-8-6-27(7-9-31)13-16-10-17(28)4-5-21(16)38-27/h4-5,10-12,18,32H,6-9,13-15H2,1-3H3,(H,30,33)(H,34,35)/t18-/m0/s1
• InChI Key: HVTUHSABWJPWNK-SFHVURJKSA-N
• Solubility: Soluble in DMSO, not in water
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: AZD-4818 is a potent antagonist of chemokine CCR1 that can be used for researching chronic obstructive pulmonary disease (COPD).
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 57.15; H, 5.68; Cl, 12.50; N, 4.94; O, 19.74
• Exact Mass: 566.15866
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Using membranes from HEK_CCR1Gqi5 cells, it was confirmed that AZD-4818, BX471, CCX354, CP481715 and PS899877 are all potent inhibitors of [125I]-CCL3 binding. In the case of AZD4818, CCX354 and CP481715, the affinity is significantly better with membranes from HEK_CCR1 cells than those from RPMI 8226 cells when tested using an unpaired t-test with Welch's correction (P < 0.05). Furthermore, there was a drastic shift in the rank order of potency between the membranes tested. With HEK_CCR1 membranes it was found that MLN3879 > CCX354 ≥ AZD4818 > CP481715 = BX471 > PS899877 while with membranes from RPMI 8226 cells we found MLN3879 > BX471 > CP481715 ≥ PS899877 > AZD4818 > CCX354. Incubation of cells with AZD-4818, BX471, CCX354, MLN-3897 or PS899877 reduced CCL3-mediated receptor internalization and led to a dose-dependent recovery of surface CCR1.; Reference: Br J Pharmacol. 2014 Nov;171(22):5127-38. https://pubmed.ncbi.nlm.nih.gov/24990525/
• In Vivo Activity: TBD
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).