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SML4220

GPR34 Antagonist, T8848

≥98% (HPLC)

Synonym(s):

N-[(2E)-3-(4′-Chloro[1,1′-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)tyrosine, (E)-3-(4-(Benzyloxy)phenyl)-2-(3-(4′-chloro-[1,1′-biphenyl]-4-yl)acrylamido)propanoic acid, T 8848, T-8848

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About This Item

Empirical Formula (Hill Notation):
C31H26ClNO4
CAS Number:
907952-06-1
Molecular Weight:
512.00
MDL number:
MFCD33548912
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Application

GPR34 Antagonist, T8848 may be used to investigate the effects of pharmacological inhibition of GPR34 on microglial dysfunction and neuroinflammation in Alzheimer’s disease (AD) mouse models.

Biochem/physiol Actions

GPR34 antagonist that potently inhibits neuroinflammation by blocking PI3K-AKT and ERK pathways, selectively reducing cytokine release.The GPR34 antagonist T8848 selectively targets G-protein coupled receptor 34 (GPR34), inhibiting LysoPS and myelin debris-induced IL-1β and IL-6 expression in microglia with high specificity. In vitro, T-8848 is applied at of 100 μg/mL, effectively reducing pro-inflammatory cytokine release. In vivo, at 10 mg/kg (i.p.) administered over 18-days in C57BL/6J mice and Gpr34-specific knockout mice (e.g., Gpr34fl/flCx3cr1CreER), it lessens neuroinflammation, demyelination, and tissue damage in models of multiple sclerosis and stroke. Mechanistically, T 8848 blocks GPR34-mediated phosphatidylinositol 3-kinase-protein kinase B (PI3K-AKT) and extracellular signal-regulated kinase (ERK) pathways, suppressing downstream inflammatory gene expression and cytokine release.

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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