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Purity: ≥98%
AZD7624 is a novel, potent and selective inhaled p38 inhibitor with anti-inflammatory activity. In order to treat lung disease effectively without producing undesirable systemic effects, inhaled medications typically aim to have a local pharmacological effect in the lung while minimizing systemic exposure. Superior pharmacodynamic lung effects and pharmacokinetic exposure are both possible with AZD7624. When compared to intravenous dosing, the lung exposure to the drug AZD7624 in rats after inhalation was five times higher. It has been demonstrated that inhaled AZD7624 significantly reduces (85%) the amount of tumor necrosis factor α (TNFα) (induced by lipopolysaccharide, or LPS), in sputum in healthy volunteers.
| Targets |
p38
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|---|---|
| ln Vitro |
AZD7624 is an inhaled p38 inhibitor that can be inhaled. With pIC50 values of 8.4, 8.1, and 9.0[1], AZD7624 inhibits LPS-induced TNFα in human mononuclear cells, whole blood, as well as in alveolar macrophages in vitro.
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| References |
| Molecular Formula |
C27H30FN5O3
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|---|---|
| Molecular Weight |
491.55720949173
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| Exact Mass |
491.23
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| Elemental Analysis |
C, 65.97; H, 6.15; F, 3.86; N, 14.25; O, 9.76
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| CAS # |
1095004-78-6
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| Related CAS # |
1095004-78-6
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C=C(C=C1F)C(=O)NC2CC2)N3C=CN=C(C3=O)NC4(CC4)C5=CC=CC=C5OCCNC
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| InChi Key |
NNKPHNTWNILINE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30FN5O3/c1-17-21(28)15-18(25(34)31-19-7-8-19)16-22(17)33-13-11-30-24(26(33)35)32-27(9-10-27)20-5-3-4-6-23(20)36-14-12-29-2/h3-6,11,13,15-16,19,29H,7-10,12,14H2,1-2H3,(H,30,32)(H,31,34)
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| Chemical Name |
N-cyclopropyl-3-fluoro-4-methyl-5-[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxopyrazin-1-yl]benzamide
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| Synonyms |
AZD-7624; AZD7624; AZD 7624
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~10 mg/mL (~18.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0343 mL | 10.1717 mL | 20.3434 mL | |
| 5 mM | 0.4069 mL | 2.0343 mL | 4.0687 mL | |
| 10 mM | 0.2034 mL | 1.0172 mL | 2.0343 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01937338 | Completed | Drug: AZD7624 Drug: Placebo |
LPS Challenge, Neutrophils | AstraZeneca | October 2013 | Phase 1 |
| NCT01754844 | Completed | Drug: AZD7624 Drug: Placebo to match |
Chronic Obstructive Pulmonary Disease (COPD) |
AstraZeneca | January 2013 | Phase 1 |
| NCT02238483 | Completed | Drug: AZD7624 1.0 mg Drug: Placebo |
Chronic Obstructive Pulmonary Disease COPD |
AstraZeneca | October 28, 2014 | Phase 2 |
| NCT01817855 | Completed | Drug: AZD7624 Drug: Placebo to match |
COPD Healthy Subjects |
AstraZeneca | September 2013 | Phase 1 |
| NCT02753764 | Completed | Drug: AZD7624 Drug: prednisone |
Corticosteroid Resistant (CR) Asthmatics |
National Jewish Health | January 2017 | Phase 2 |
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