| Bioactivity | SM-324405 is a TLR7 agonistic antedrug (EC50 = 50 nM), with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunotherapy of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment[1][2][3]. | ||||||||||||
| Invitro | SM-324405 is a novel candidate for immunotherapy of allergic diseases[1]. | ||||||||||||
| In Vivo | SM-324405 (9e, intratracheal administration) effectively inhibits allergen-induced airway inflammation without inducing cytokines systemically[1].SM-324405 is metabolized to the corresponding acid in human plasma with t1/2 of 2.6 min[1][2]. | ||||||||||||
| Name | SM-324405 | ||||||||||||
| CAS | 677773-91-0 | ||||||||||||
| Formula | C19H23N5O4 | ||||||||||||
| Molar Mass | 385.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ayumu Kurimoto, et al. Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept. J Med Chem. 2010 Apr 8;53(7):2964-72. [2]. M Biffen, et al. Biological characterization of a novel class of toll-like receptor 7 agonists designed to have reduced systemic activity. Br J Pharmacol. 2012 May;166(2):573-86. [3]. Sang Nam Lee, et al. Chemical Strategies to Enhance the Therapeutic Efficacy of Toll-like Receptor Agonist Based Cancer Immunotherapy. Acc Chem Res. 2020 Oct 20;53(10):2081-2093. |