Free shipping on all orders over $ 500

CNS 5161 

Cat. No. M28659
CNS 5161  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

Chemical Information
Molecular Weight 351.92
Formula C16H18ClN3S2
CAS Number 160754-76-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Colm J McGinnity, et al. EJNMMI Res. Simplifying [18F]GE-179 PET: are both arterial blood sampling and 90-min acquisitions essential?

[2] Anat Biegon, et al. Synapse. In vitro and in vivo characterization of [3H]CNS-5161--a use-dependent ligand for the N-methyl-D-aspartate receptor in rat brain

[3] Thomas Forst, et al. Br J Clin Pharmacol. Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain

[4] Wojciech Danysz, et al. Neurotox Res. Neuroprotective potential of ionotropic glutamate receptor antagonists

[5] M R Walters, et al. Br J Clin Pharmacol. Early clinical experience with the novel NMDA receptor antagonist CNS 5161

Related GluR Products
LY367385 hydrochloride

LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist, with an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a.

PDZ1 Domain inhibitor peptide

PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95).

CALP1

CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site.

NT 13

NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide.

Tat-NR2Baa

Tat-NR2BAA is the control peptide of Tat-NR2B9c, inactive.

  Catalog
Abmole Inhibitor Catalog




Keywords: CNS 5161  supplier, GluR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.