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BRL 44408 Maleate is a potent α2A-adrenoceptor antagonist with antidepressant and analgesic activity that reduces lipopolysaccharide (LPS)-induced expression and attenuates endogenous lipopolysaccharide-induced acute lung injury through inhibition of the mitogen-activated protein kinase kinase/extracellularly regulated protein kinase signaling pathway in mice.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $166 | In Stock | |
10 mg | $297 | In Stock | |
25 mg | $492 | In Stock | |
50 mg | $717 | In Stock | |
100 mg | $1,056 | In Stock |
Description | BRL 44408 Maleate is a potent α2A-adrenoceptor antagonist with antidepressant and analgesic activity that reduces lipopolysaccharide (LPS)-induced expression and attenuates endogenous lipopolysaccharide-induced acute lung injury through inhibition of the mitogen-activated protein kinase kinase/extracellularly regulated protein kinase signaling pathway in mice. |
Targets&IC50 | α2A-adrenoceptor:7.9 nM (K (B)), α2A-adrenoceptor:8.5 nM (Ki) |
In vitro | BRL 44408 Maleate Salt, a potent (Ki=8.5 nM) and selective (>50-fold) alpha2A-adrenoceptor antagonist (K(B)=7.9 nM). [1] |
In vivo | In rats, BRL 44408 Maleate Salt penetrated the central nervous system resulting in peak brain and plasma concentrations of 586 ng/g and 1124 ng/ml, respectively. In a pharmacodynamic assay, pretreatment with BRL 44408 Maleate Salt to rats responding under a fixed-ratio 30 operant response paradigm resulted in a rightward shift of the clonidine dose-response curve, an effect indicative of alpha2-adrenoceptor antagonism in vivo. [1] |
Alias | BRL44408 Maleate |
Molecular Weight | 331.37 |
Formula | C17H21N3O4 |
Cas No. | 681806-46-2 |
Smiles | C(=C\C(O)=O)\C(O)=O.CC1C=2C(CN1CC=3NCCN3)=CC=CC2 |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL(60.36 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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