| Size | Price | Stock | Qty |
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| ln Vitro |
AZD8848 demonstrates strong anti-TLR7 action, with pEC50 values for human TLR7 and TLR7-adsorbed cells being 7.0 and 6.6, respectively [1]. Regardless of whether PHA polyclonal or inhibitory presentation is used to boost T cells, AZD8848 has an EC50 of 4 nM when generating IFNα in human peripheral blood mononuclear cells and an IC50 of 0.2-1.0 nM when blocking IL-5 [1]. Locally inhibiting Th2 responses, AZD8848 is a strong and selective prodrug of TLR7 agonist [1]. AZD8848 has no anti-human TLR8 or anti-tLR1 action [1].
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| ln Vivo |
In Brown's Norway, AZD8848 (0.1–1 mg/kg; intratracheal) exhibits favorable pharmacokinetics [1]. Ovalbumin (OVA) response is inhibited by AZD8848 (0.3 mg/kg; intratracheal) Response model
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| Animal Protocol |
Animal/Disease Models: Brown Norway rat allergy model [1]
Doses: 0.1 mg/kg, 1 mg/kg Route of Administration: intratracheal ( 24 hrs (hrs (hours)) before OVA challenge and 24 hrs (hrs (hours)) after OVA challenge) Experimental Results: Inhibited OVA challenge in a dose-dependent manner. Animal/Disease Models: Norwegian brown rat[1] Doses: 0.3 mg/kg (pharmacokinetic/PK/PK analysis) Mode of Route of Administration: Intratracheal Experimental Results: Very short half-life in rat blood (0.2 minutes), with a slow decline thereafter, levels Above 1000 nmol/kg for more than 5 hrs (hrs (hours)). |
| References | |
| Additional Infomation |
AZD-8848 is under investigation in clinical trial NCT01818869 (To Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Doses AZD8848 in Healthy Subjects).
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| Molecular Formula |
C29H43N7O5
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|---|---|
| Molecular Weight |
569.695626497269
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| Exact Mass |
569.332
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| CAS # |
866269-28-5
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| PubChem CID |
11592228
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| Appearance |
White to off-white solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
41
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| Complexity |
802
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FEFIBEHSXLKJGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H43N7O5/c1-3-4-16-41-28-32-26(30)25-27(33-28)36(29(38)31-25)13-7-12-35(11-6-10-34-14-17-40-18-15-34)21-23-9-5-8-22(19-23)20-24(37)39-2/h5,8-9,19H,3-4,6-7,10-18,20-21H2,1-2H3,(H,31,38)(H2,30,32,33)
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| Chemical Name |
methyl 2-[3-[[3-(6-amino-2-butoxy-8-oxo-7H-purin-9-yl)propyl-(3-morpholin-4-ylpropyl)amino]methyl]phenyl]acetate
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| Synonyms |
AZD8848 AZD 8848 AZD-8848
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| HS Tariff Code |
2934.99.9001
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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 : ~25 mg/mL (~43.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.39 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 25.0 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: 2.5 mg/mL (4.39 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7553 mL | 8.7765 mL | 17.5531 mL | |
| 5 mM | 0.3511 mL | 1.7553 mL | 3.5106 mL | |
| 10 mM | 0.1755 mL | 0.8777 mL | 1.7553 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 |
| NCT01818869 | COMPLETED | Drug: AZD8848 Drug: Placebo to match AZD8848 |
Healthy Subjects Safety, Tolerability, |
AstraZeneca | 2014-01 | Phase 1 |
| NCT01205867 | COMPLETED | Drug: AZD8848 | Butyrylcholinesterase Deficiency | AstraZeneca | 2010-09 | Phase 1 |
| NCT01203124 | COMPLETED | Drug: AZD8848 Drug: Placebo |
Healthy Volunteers | AstraZeneca | 2010-11 | Phase 1 |
| NCT00770003 | COMPLETED | Drug: AZD8848 Drug: Placebo |
Allergic Rhinitis | AstraZeneca | 2008-09 | Phase 1 |
| NCT00688779 | COMPLETED | Drug: AZD8848 Drug: Placebo |
Allergic Rhinitis Healthy |
AstraZeneca | 2008-01 | Phase 1 |
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