BRL-44408 maleate
Based on 1 Customer Validation
BRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain.
For research use only. We do not sell to patients.
- Purity: 99.0%
- CAS No.: 681806-46-2
- Formula: C17H21N3O4
- Molecular Weight:331.37
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Ki: 8.5 nM (α2A-adrenoceptor)[1]
BRL-44408 maleate (0-12.5 h) can inhibit the secretion of proinflammatory cytokines and the phosphorylation of ERK1/2, p38MAPK and p65 in LPS (HY-D1056)-induced NR8383 rat alveolar macrophages, with no effect on the activation of JNK or PKA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BRL-44408 (10 mg/kg; subcutaneous injection; single administration) maleate significantly elevates extracellular norepinephrine (up to 204%), dopamine (up to 110%) and acetylcholine (up to 75%) levels in the medial prefrontal cortex (mPFC) of rats for at least 3.5 hours post-administration, without altering serotonin levels[2].
BRL-44408 maleate (3-30 mg/kg; i.p.; administered once at 24 h, 5 h and 1 h prior to testing, for a total of 3 times) exerts significant antidepressant-like effects in the forced swimming test in rats, reducing the immobility time by 30% (10 mg/kg) and 49% (30 mg/kg), while increasing the climbing time by 48% (10 mg/kg) and 107% (30 mg/kg)[2].
BRL-44408 maleate (10-30 mg/kg; i.p.; single administration; pretreated 20 minutes before testing) exerts significant antidepressant-like effects in the rat procedure-induced polydipsia test, reducing the additional water intake by 34% (17 mg/kg) and 44% (30 mg/kg), respectively[2].
BRL-44408 maleate (1-30 mg/kg; i.p.; single administration; pretreated 60 minutes prior to PPQ administration) exerts significant analgesic effects in a mouse PPQ visceral pain model, reversing somatic stretching behaviors by 32% (10 mg/kg) and 52% (30 mg/kg), respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 260-280 g, ARDS induced via cecal ligation puncture)[1]
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Dosage:5 mg/kg
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Administration:i.p.; single dose (administered 5 hr after CLP)
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Result:Significantly reduced CLP-induced lung wet/dry weight ratio.
Significantly decreased CLP-induced lung injury scores.
Significantly reduced CLP-induced CD68-positive macrophage infiltration in lung tissue.
Significantly decreased serum levels of TNF-α, IL-6, and CXCL2/MIP-2; no significant effect on serum IL-10 levels.
Significantly reduced lung tissue mRNA expression of TNF-α, IL-6, and CXCL2/MIP-2 post-CLP; no significant effect on lung tissue IL-10 mRNA levels.
Markedly inhibited CLP-induced phosphorylation of ERK1/2, p38MAPK, and p65 in lung tissue; no effect on phosphorylation of JNK or PKA.
Increased 7-day survival rate by approximately 20% compared to CLP controls, with no statistically significant difference between groups.
Chemical Information
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CAS No. 681806-46-2
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Appearance Solid
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Molecular Weight 331.37
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Formula C17H21N3O4
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Color Light brown to brown
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SMILES
CC1N(CC2=NCCN2)CC3=C1C=CC=C3.O=C(O)/C=C\C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL (75.44 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Cong Z, et al. α2A -AR antagonism by BRL-44408 maleate attenuates acute lung injury in rats with downregulation of ERK1/2, p38MAPK, and p65 pathway. J Cell Physiol. 2020;235(10):6905-6914. [Content Brief]
[2]. Dwyer JM, et al. Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism. Int J Neuropsychopharmacol. 2010;13(9):1193-1205. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0178 mL | 15.0889 mL | 30.1777 mL | 75.4444 mL |
| 5 mM | 0.6036 mL | 3.0178 mL | 6.0355 mL | 15.0889 mL | |
| 10 mM | 0.3018 mL | 1.5089 mL | 3.0178 mL | 7.5444 mL | |
| 15 mM | 0.2012 mL | 1.0059 mL | 2.0118 mL | 5.0296 mL | |
| 20 mM | 0.1509 mL | 0.7544 mL | 1.5089 mL | 3.7722 mL | |
| 25 mM | 0.1207 mL | 0.6036 mL | 1.2071 mL | 3.0178 mL | |
| 30 mM | 0.1006 mL | 0.5030 mL | 1.0059 mL | 2.5148 mL | |
| 40 mM | 0.0754 mL | 0.3772 mL | 0.7544 mL | 1.8861 mL | |
| 50 mM | 0.0604 mL | 0.3018 mL | 0.6036 mL | 1.5089 mL | |
| 60 mM | 0.0503 mL | 0.2515 mL | 0.5030 mL | 1.2574 mL |
BRL-44408 maleate Related Classifications
HY-12716A Related Classifications
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