AZD-4818

AZD-4818 is a chemokine CCR1 antagonist that is used for the treatment of chronic obstructive pulmonary disease.

Product information

CAS Number: 1003566-93-5

Molecular Weight: 567.46

Formula: C27H32Cl2N2O7

Chemical Name: (S)-2-(2-chloro-5-(3-(5-chloro-3H-spiro[benzofuran-2, 4'-piperidin]-1'-yl)-2-hydroxypropoxy)-4-(methylcarbamoyl)phenoxy)

Smiles: CC(C)(OC1=CC(OC[C@@H](O)CN2CCC3(CC4=CC(Cl)=CC=C4O3)CC2)=C(C=C1Cl)C(=O)NC)C(O)=O

InChiKey: HVTUHSABWJPWNK-SFHVURJKSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Gilchrist A, Gauntner TD, Fazzini A, Alley KM, Pyen DS, Ahn J, Ha SJ, Willett A, Sansom SE, Yarfi JL, Bachovchin KA, Mazzoni MR, Merritt JR. Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays. Br J Pharmacol. 2014 Nov;171(22):5127-38. doi: 10.1111/bph.12835. PubMed PMID: 24990525; PubMed Central PMCID: PMC4253460.
2. Olsson B, Borgström L, Lundbäck H, Svensson M. Validation of a general in vitro approach for prediction of total lung deposition in healthy adults for pharmaceutical inhalation products. J Aerosol Med Pulm Drug Deliv. 2013 Dec;26(6):355-69. doi: 10.1089/jamp.2012.0986. Epub 2013 Feb 19. PubMed PMID: 23421897.
3. Gladue RP, Brown MF, Zwillich SH. CCR1 antagonists: what have we learned from clinical trials. Curr Top Med Chem. 2010;10(13):1268-77. Review. PubMed PMID: 20536425.
4. Kerstjens HA, Bjermer L, Eriksson L, Dahlström K, Vestbo J. Tolerability and efficacy of inhaled AZD4818, a CCR1 antagonist, in moderate to severe COPD patients. Respir Med. 2010 Sep;104(9):1297-303. doi: 10.1016/j.rmed.2010.04.010. Epub 2010 May 13. PubMed PMID: 20466530.
5. Norman P. AZD-4818, a chemokine CCR1 antagonist: WO2008103126 and WO2009011653. Expert Opin Ther Pat. 2009 Nov;19(11):1629-33. doi: 10.1517/13543770903118996. PubMed PMID: 19586423.

Products are for research use only. Not for human use.