Date published: 2025-12-19

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BRL 44408 MALEATE (CAS 118343-19-4)

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Application:
BRL 44408 MALEATE is a selective α2A-AR antagonist
CAS Number:
118343-19-4
Molecular Weight:
331.37
Molecular Formula:
C13H17N3•C4H4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Zinc finger BTB domain containing (ZBTB) proteins are a family of transcription factors characterized by a distinct combination of zinc finger motifs and a BTB (Broad-Complex, Tramtrack, and Bric à brac) domain. The zinc finger motifs enable DNA binding, allowing these proteins to regulate the expression of target genes, while the BTB domain facilitates protein-protein interactions, often leading to the formation of multiprotein complexes. ZBTB proteins are involved in a wide range of cellular processes, including cell cycle regulation, differentiation, and development. The diverse functions of ZBTB proteins often involve interactions with chromatin remodeling complexes, influencing epigenetic landscapes. ZBTB proteins, such as ZBTB7A (Pokemon), play a significant role in oncogenesis, highlighting their importance in cell proliferation and apoptosis. The intricate balance in ZBTB signaling is crucial for maintaining normal cellular function, and dysregulation of this balance can lead to various pathologies. Targeting Zinc finger BTB domain containing (ZBTB) proteins for disruption or inhibition is a sophisticated approach that aims to modulate the function of these transcription factors, which play pivotal roles in numerous cellular processes. Given the diversity of functions ZBTB proteins perform, from gene regulation to involvement in development and cell differentiation, their inhibition or disruption can have far-reaching cellular consequences. Strategies for targeting ZBTB proteins would likely focus on disrupting their DNA-binding capability or interfering with their interactions with other proteins, particularly within chromatin remodeling complexes.


BRL 44408 MALEATE (CAS 118343-19-4) References

  1. Different alpha(2) adrenoceptor subtypes control noradrenaline release and cell firing in the locus coeruleus of wildtype and monoamine oxidase-A knockout mice.  |  Owesson, CA., et al. 2003. Eur J Neurosci. 18: 34-42. PMID: 12859335
  2. Pivotal role of the alpha(2A)-adrenoceptor in producing inflammation and organ injury in a rat model of sepsis.  |  Miksa, M., et al. 2009. PLoS One. 4: e5504. PMID: 19430535
  3. Antagonism of alpha2A-adrenoceptor: a novel approach to inhibit inflammatory responses in sepsis.  |  Zhang, F., et al. 2010. J Mol Med (Berl). 88: 289-96. PMID: 19894027
  4. Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism.  |  Dwyer, JM., et al. 2010. Int J Neuropsychopharmacol. 13: 1193-205. PMID: 20047711
  5. Centhaquin antinociception in mice is mediated by α2A- and α2B- but not α2C-adrenoceptors.  |  Bhalla, S., et al. 2013. Eur J Pharmacol. 715: 328-36. PMID: 23712005
  6. α2A-adrenoceptors, but not nitric oxide, mediate the peripheral cardiac sympatho-inhibition of moxonidine.  |  Cobos-Puc, LE., et al. 2016. Eur J Pharmacol. 782: 35-43. PMID: 27112661
  7. The effects of progesterone on the alpha2-adrenergic receptor subtypes in late-pregnant uterine contractions in vitro.  |  Hajagos-Tóth, J., et al. 2016. Reprod Biol Endocrinol. 14: 33. PMID: 27301276
  8. Further analysis of the inhibition by agmatine on the cardiac sympathetic outflow: Role of the α2-adrenoceptor subtypes.  |  Cobos-Puc, L., et al. 2017. Eur J Pharmacol. 805: 75-83. PMID: 28315344
  9. [BRL-44408 maleate, the antagonist of α2A-adrenoceptor, attenuates endogenous lipopolysacchride-induced acute lung injury through inhibiting the mitogen-activated protein kinase kinase/extracellular regulated protein kinases signaling pathway in mice].  |  Lyu, X., et al. 2018. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 30: 101-106. PMID: 29402356
  10. α2A -AR antagonism by BRL-44408 maleate attenuates acute lung injury in rats with downregulation of ERK1/2, p38MAPK, and p65 pathway.  |  Cong, Z., et al. 2020. J Cell Physiol. 235: 6905-6914. PMID: 32003020
  11. Dexmedetomidine attenuates sepsis-associated inflammation and encephalopathy via central α2A adrenoceptor.  |  Mei, B., et al. 2021. Brain Behav Immun. 91: 296-314. PMID: 33039659
  12. Subtype classification of presynaptic alpha 2-adrenoceptors.  |  Alberts, P. 1993. Gen Pharmacol. 24: 1-8. PMID: 8387042
  13. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain.  |  Meana, JJ., et al. 1996. Eur J Pharmacol. 312: 385-8. PMID: 8894622

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

BRL 44408 MALEATE, 10 mg

sc-217791
10 mg
$200.00