AZD-1236
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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.


Chemical Structure

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AZD-1236
CAS# 459814-89-2 (free base)

Theoretical Analysis

MedKoo Cat#: 573391
Name: AZD-1236
CAS#: 459814-89-2 (free base)
Chemical Formula: C15H19ClN4O5S
Exact Mass: 402.08
Molecular Weight: 402.850
Elemental Analysis: C, 44.72; H, 4.75; Cl, 8.80; N, 13.91; O, 19.86; S, 7.96

Price and Availability

Size Price Availability Quantity
1mg USD 90 Ready to Ship
5mg USD 350 Ready to Ship
10mg USD 550 Ready to Ship
25mg USD 950 Ready to Ship
50mg USD 1650 Ready to Ship
100mg USD 2950 Ready to Ship
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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

More Info:

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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.