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

Ro 25-6981 Maleate 

Cat. No.: HY-13993A Purity: 98.49% ee.: 99.29%
Handling Instructions

Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.

For research use only. We do not sell to patients.
Ro 25-6981 Maleate Chemical Structure

Ro 25-6981 Maleate Chemical Structure

CAS No. : 1312991-76-6

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10 mM * 1 mL in DMSO USD 106 In-stock
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Other Forms of Ro 25-6981 Maleate:

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  • References

Description

Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. IC50 value: 9 nM [1] Target: NMDA receptor subtype of NR1C & NR2B in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2]. in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3].

References
Molecular Weight

455.54

Formula

C₂₆H₃₃NO₆

CAS No.

1312991-76-6

SMILES

OC1=CC=C([[email protected]](O)[[email protected]@H](C)CN2CCC(CC3=CC=CC=C3)CC2)C=C1.O=C(O)/C=C\C(O)=O

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

Solvent & Solubility

DMSO: ≥ 61 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Ro 25-6981 Maleate
Cat. No.:
HY-13993A
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