WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206473
CAS#: 878385-84-3
Description: AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD. AZD-5069 was shown to inhibit binding of radiolabeled CXCL8 to human CXCR2 with a pIC50 value of 9.1. Furthermore, AZD5069 inhibited neutrophil chemotaxis, with a pA2 of approximately 9.6, and adhesion molecule expression, with a pA2 of 6.9, in response to CXCL1. AZD5069 was a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics. AZD-5069 is also potential useful for patient in inflammatory conditions.
MedKoo Cat#: 206473
Name: AZD-5069
CAS#: 878385-84-3
Chemical Formula: C18H22F2N4O5S2
Exact Mass: 476.09997
Molecular Weight: 476.51
Elemental Analysis: C, 45.37; H, 4.65; F, 7.97; N, 11.76; O, 16.79; S, 13.46
Synonym: AZD-5069; AZD 5069; AZD5069.
IUPAC/Chemical Name: N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide
InChi Key: QZECRCLSIGFCIO-RISCZKNCSA-N
InChi Code: InChI=1S/C18H22F2N4O5S2/c1-11(14(26)9-25)29-16-8-15(23-31(27,28)24-6-3-7-24)21-18(22-16)30-10-12-4-2-5-13(19)17(12)20/h2,4-5,8,11,14,25-26H,3,6-7,9-10H2,1H3,(H,21,22,23)/t11-,14+/m1/s1
SMILES Code: O=S(N1CCC1)(NC2=NC(SCC3=CC=CC(F)=C3F)=NC(O[C@H](C)[C@@H](O)CO)=C2)=O
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 476.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: De Soyza A, Pavord I, Elborn JS, Smith D, Wray H, Puu M, Larsson B, Stockley
R. A randomised, placebo-controlled study of the CXCR2 antagonist AZD5069 in
bronchiectasis. Eur Respir J. 2015 Sep 4. pii: ERJ-00148-2015. doi:
10.1183/13993003.00148-2015. [Epub ahead of print] PubMed PMID: 26341987.
2: Jurcevic S, Humfrey C, Uddin M, Warrington S, Larsson B, Keen C. The effect of
a selective CXCR2 antagonist (AZD5069) on human blood neutrophil count and innate
immune functions. Br J Clin Pharmacol. 2015 Jul 15. doi: 10.1111/bcp.12724. [Epub
ahead of print] PubMed PMID: 26182832.
3: Nicholls DJ, Wiley K, Dainty I, MacIntosh F, Phillips C, Gaw A, Mårdh CK.
Pharmacological characterization of AZD5069, a slowly reversible CXC chemokine
receptor 2 antagonist. J Pharmacol Exp Ther. 2015 May;353(2):340-50. doi:
10.1124/jpet.114.221358. Epub 2015 Mar 3. PubMed PMID: 25736418.
4: Kirsten AM, Förster K, Radeczky E, Linnhoff A, Balint B, Watz H, Wray H,
Salkeld L, Cullberg M, Larsson B. The safety and tolerability of oral AZD5069, a
selective CXCR2 antagonist, in patients with moderate-to-severe COPD. Pulm
Pharmacol Ther. 2015 Apr;31:36-41. doi: 10.1016/j.pupt.2015.02.001. Epub 2015 Feb
11. PubMed PMID: 25681277.
