SML2121
A-33
≥98% (HPLC)
别名:
2-(4-{[2-(5-Chlorothiophen-2-yl)-5-ethyl-6-methylpyrimidin-4-yl]amino}phenyl)acetic acid, 2-[4-[[2-(5-Chloro-2-thienyl)-5-ethyl-6-methyl-pyrimidin-4-yl]amino]phenyl]acetic acid, 4-[[2-(5-Chloro-2-thienyl)-5-ethyl-6-methyl-4-pyrimidinyl]amino]-benzeneacetic acid, A33
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关于此项目
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(O)CC1=CC=C(NC2=NC(C3=CC=C(Cl)S3)=NC(C)=C2CC)C=C1
InChI key
FDVSPBLZPJMXFV-UHFFFAOYSA-N
Biochem/physiol Actions
A-33 (A33) is a potent and selective catalytic site-targeting PDE4B inhibitor (IC50 = 15 nM/PDE4B vs. 1.7 μM/PDE4D) that effectively prevents PDE4B-medicated cellular cAMP hydrolysis (150%/320% increased cAMP level with 100 nM/1 μM A-33 pre-treament in murine hippocampal HT-22 cells following 10 nM isoproterenol stimulation) in vitro and inhibits LPS-induced TNF-α production in mice in vivo (ID50 = 14 mg/kg p.o.). When administered via intraperitoneal injection, A-33 improves cognitive function in a rat model of traumatic brain injury (0.3 mg/kg i.p.) and exhibits antidepressant property in mice (0.3-1 mg/kg i.p.) in vivo.
Orally acive, potent and selective catalytic site-targeting PDE4B inhibitor with anti-inflammatory, antidepressant, and cognition-improving efficacy in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3