1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR

IC87201 

Cat. No.: HY-100457 Purity: 95.53%
Handling Instructions

IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

For research use only. We do not sell to patients.

IC87201 Chemical Structure

IC87201 Chemical Structure

CAS No. : 866927-10-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 286 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

In Vitro

IC87201 (500-1800 μM) does not inhibit any of the probe-PDZ interactions involving PDZ1, PDZ2, PDZ3 of PSD-95 or nNOS-PDZ, or bind the canonical PDZ ligand binding sites. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe[1]. IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation relative to vehicle, in cultured hippocampal neurons[2]. IC87201 (10 and 100 nM) attenuats NMDA/glycine-induced decreases in neurite outgrowth. IC87201 dose-dependently reduces NMDA-induced cGMP production in primary hippocampal neurons (DIV 14-21) with an IC50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons[3].

In Vivo

IC87201 (1, 4 and 10 mg/kg, i.p.) does not produce impairment in either spatial working memory or source memory[2]. IC87201 (1 mg/kg) is effective in treating NMDA-induced thermal hyperalgesia in mice, with a corresponding peak plasma level of 55 ng/mL (or 0.2 μM)[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (90.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2347 mL 16.1734 mL 32.3468 mL
5 mM 0.6469 mL 3.2347 mL 6.4694 mL
10 mM 0.3235 mL 1.6173 mL 3.2347 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

MK-801 is dissolved in saline and administered intraperitoneally (i.p.) in a within subjects dosing paradigm in order of increasing dose (0.1, 0.2, and 0.3 mg/kg). IC87201 (1, 4 and 10 mg/kg) and ZL006 (10 mg/kg) are dissolved in a vehicle containing 3% DMSO with the remaining 97% comprised of 1:1:18 of emulphor:ethanol:0.9% NaCl. Active compounds are compared with equivalent volumes of the appropriate vehicle in each case. MK-801, IC87201, and ZL006 are administered 30 min prior to behavioral testing. All drugs are administered intraperitoneally (i.p.) in a volume of 1 mL/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

309.15

Formula

C₁₃H₁₀Cl₂N₄O

CAS No.

866927-10-8

SMILES

OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C3N=NNC3=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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IC87201
Cat. No.:
HY-100457
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IC87201

Cat. No.: HY-100457