WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 573391
CAS#: 459814-89-2 (free base)
Description: AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished macrophage infiltration into BAL fluid induced by tobacco smoke inhalation in the mouse.
MedKoo Cat#: 573391
Name: AZD-1236
CAS#: 459814-89-2 (free base)
Chemical Formula: C15H19ClN4O5S
Exact Mass: 402.0765
Molecular Weight: 402.85
Elemental Analysis: C, 44.72; H, 4.75; Cl, 8.80; N, 13.91; O, 19.86; S, 7.96
Related CAS #: AZD1236 HCl 459814-89-2 (free base) 459814-90-5 (R-isomer)
Synonym: AZD-1236, AZD1236, AZD 1236;
IUPAC/Chemical Name: 2,4-Imidazolidinedione, 5-(((4-((5-chloro-2-pyridinyl)oxy)-1-piperidinyl)sulfonyl)methyl)-5-methyl-, (5S)-
InChi Key: SFJFBTPHDHUUPU-OAHLLOKOSA-N
InChi Code: 1S/C15H19ClN4O5S/c1-15(13(21)18-14(22)19-15)9-26(23,24)20-6-4-11(5-7-20)25-12-3-2-10(16)8-17-12/h2-3,8,11H,4-7,9H2,1H3,(H2,18,19,21,22)/t15-/m1/s1
SMILES Code: O=C1NC([C@@](C)(CS(=O)(N2CCC(OC3=NC=C(Cl)C=C3)CC2)=O)N1)=O
Appearance: 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
Shelf Life: >3 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
| Biological target: | AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively). |
| In vitro activity: | TBD |
| In vivo activity: | TBD |
The following data is based on the product molecular weight 402.85 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 |
| Formulation protocol: | TBD |
| In vitro protocol: | TBD |
| In vivo protocol: | TBD |
1: Dahl R, Titlestad I, Lindqvist A, Wielders P, Wray H, Wang M, Samuelsson V, Mo J, Holt A. Effects of an oral MMP-9 and -12 inhibitor, AZD1236, on biomarkers in moderate/severe COPD: a randomised controlled trial. Pulm Pharmacol Ther. 2012 Apr;25(2):169-77. doi: 10.1016/j.pupt.2011.12.011. Epub 2012 Feb 1. PubMed PMID: 22306193.
2: Magnussen H, Watz H, Kirsten A, Wang M, Wray H, Samuelsson V, Mo J, Kay R. Safety and tolerability of an oral MMP-9 and -12 inhibitor, AZD1236, in patients with moderate-to-severe COPD: a randomised controlled 6-week trial. Pulm Pharmacol Ther. 2011 Oct;24(5):563-70. doi: 10.1016/j.pupt.2011.05.003. Epub 2011 May 23. PubMed PMID: 21624491.
