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Chemical Structure| 894002-50-7 Chemical Structure| 894002-50-7

Structure of LDN-212320
CAS No.: 894002-50-7

Chemical Structure| 894002-50-7

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LDN-212320 is a glutamate transporter EAAT2 activator and enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

Synonyms: OSU-0212320; LDN-0212320; LDN-0212320 Maleate

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Product Details of LDN-212320

CAS No. :894002-50-7
Formula : C17H15N3S
M.W : 293.39
SMILES Code : CC1=CC=CC=C1CSC2=NN=C(C3=NC=CC=C3)C=C2
Synonyms :
OSU-0212320; LDN-0212320; LDN-0212320 Maleate
MDL No. :MFCD05960679
InChI Key :DUUQLWDHNYFUPP-UHFFFAOYSA-N
Pubchem ID :7207425

Safety of LDN-212320

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

Description
LDN-212320 functions as an activator for the glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) at the translational level. It alleviates nociceptive pain through the upregulation of astroglial GLT-1 expression in the hippocampus and anterior cingulate cortex (ACC)[1][2].

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6NCrl mice Photothrombotic focal ischemia model Intraperitoneal injection 40-100 mg/kg Single injection, 24 hours or 2 hours before inducing focal ischemia To evaluate the effects of LDN on stroke-associated brain injury. Male mice treated with LDN showed upregulated GLT-1 protein levels, significantly smaller infarct size, and better sensorimotor performance compared to vehicle-treated males. In contrast, female mice treated with LDN did not show upregulated GLT-1 protein levels, and there was no difference in infarct size or sensorimotor performance between vehicle- and LDN-treated females. Brain Sci. 2021 Jan 8;11(1):76
Male FVB/N mice Healthy wild-type mice Intraperitoneal injection 40 mg/kg Single injection LDN significantly increased total GLT-1 expression in the hippocampus, cortex, and striatum but had minimal impact on the clearance rate of extracellular glutamate following evoked synaptic release. Front Cell Neurosci. 2021 Mar 26;15:661412
C57BL/6J mice CFA-induced chronic inflammatory pain model Intraperitoneal injection 20 mg/kg Administered 24 h prior, duration of 7 days LDN-212320 significantly attenuated CFA-induced tactile allodynia and thermal hyperalgesia by upregulating astroglial GLT-1 and CX43 expression and decreasing microglial activation in the hippocampus and ACC. Brain Sci. 2023 May 16;13(5):807

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.04mL

3.41mL

1.70mL

34.08mL

6.82mL

3.41mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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