WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522630
CAS#: 866269-28-5 (free base)
Description: AZD8848, also known as DSP-3025, is a topical Toll-like receptor 7 agonist (TLR7 agonist) under development for seasonal allergic rhinitis. Repeated administration of AZD8848 activated TLR7 and produced IFN-induced effects. This was associated with a sustained reduction in allergen responsiveness. TLR agonists herald promising results for allergen immunotherapy of patients with allergic rhinitis and asthma.
Hodoodo Cat#: H522630
Name: AZD8848
CAS#: 866269-28-5 (free base)
Chemical Formula: C29H43N7O5
Exact Mass: 569.33
Molecular Weight: 569.707
Elemental Analysis: C, 61.14; H, 7.61; N, 17.21; O, 14.04
Synonym: AZD8848; AZD-8848; AZD 8848; DSP-3025; DSP 3025; DSP3025.
IUPAC/Chemical Name: methyl 2-(3-(((3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl)(3-morpholinopropyl)amino)methyl)phenyl)acetate
InChi Key: FEFIBEHSXLKJGI-UHFFFAOYSA-N
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)
SMILES Code: O=C(OC)CC1=CC=CC(CN(CCCN2C(NC3=C(N)N=C(OCCCC)N=C23)=O)CCCN4CCOCC4)=C1
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, 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
More Info: Related: 866269-28-5 (AZD8848 free base) 1162113-73-6 (AZD8848 HCl salt) Note: Structrue was from: Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma. Keith Biggadike, Mahbub Ahmed, Doug I. Ball, Diane M. Coe, Deidre A. Dalmas Wilk, Chris D. Edwards, Bob H. Gibbon, Charlotte J. Hardy, Stephen A. Hermitage, Joanne O. Hessey, Aimee E. Hillegas, Stephen C. Hughes, Linos Lazarides, Xiao Q. Lewell, Amanda Lucas, David N. Mallett, Mark A. Price, Fiona M. Priest, Diana J. Quint, Poonam Shah, Anesh Sitaram, Stephen A. Smith, Richard Stocker, Naimisha A. Trivedi, Daphne C. Tsitoura, and Victoria Weller Publication Date (Web): February 10, 2016 (Drug Annotation). DOI: 10.1021/acs.jmedchem.5b01647
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The following data is based on the product molecular weight 569.71 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Aryan Z, Rezaei N. Toll-like receptors as targets for allergen immunotherapy.
Curr Opin Allergy Clin Immunol. 2015 Dec;15(6):568-74. doi:
10.1097/ACI.0000000000000212. PubMed PMID: 26418475.
2: Greiff L, Ahlström-Emanuelsson C, Alenäs M, Almqvist G, Andersson M, Cervin A,
Dolata J, Lindgren S, Mårtensson A, Young B, Widegren H. Biological effects and
clinical efficacy of a topical Toll-like receptor 7 agonist in seasonal allergic
rhinitis: a parallel group controlled phase IIa study. Inflamm Res. 2015
Nov;64(11):903-15. doi: 10.1007/s00011-015-0873-2. Epub 2015 Sep 5. PubMed PMID:
26342289.
3: Aryan Z, Holgate ST, Radzioch D, Rezaei N. A new era of targeting the ancient
gatekeepers of the immune system: toll-like agonists in the treatment of allergic
rhinitis and asthma. Int Arch Allergy Immunol. 2014;164(1):46-63. doi:
10.1159/000362553. Epub 2014 May 21. Review. PubMed PMID: 24853609.
4: Greiff L, Cervin A, Ahlström-Emanuelsson C, Almqvist G, Andersson M, Dolata J,
Eriksson L, Högestätt E, Källén A, Norlén P, Sjölin IL, Widegren H. Repeated
intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis.
Respir Res. 2012 Jun 22;13:53. doi: 10.1186/1465-9921-13-53. PubMed PMID:
22726593; PubMed Central PMCID: PMC3487914.
