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Cat. No.: HY-181977

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RPI-GLYT2-82

Name: RPI-GLYT2-82
Brand: MedChemExpress
SKU: HY-181977
Price: 280.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC₅₀ value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC₅₀ values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.

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

Purity: 99.12%
Formula: C₂₄H₃₀ClN₃O₃
Molecular Weight:443.97

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

RPI-GLYT2-82 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

GlyT2

544 nM (IC₅₀)

5-HT_2A Receptor

1.9 μM (IC₅₀)

All GlyT Isoforms :

GlyT1
GlyT2

All 5-HT Receptor Isoforms :

In Vivo

RPI-GLYT2-82 (50-150 mg/kg, i.p., single administration) produces dose-dependent analgesic effects in mouse chronic constriction injury (CCI) and partial sciatic nerve ligation (PSNL) neuropathic pain models^[1].

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

Animal Model:

C57BL/6 (male, female, 6 weeks old at arrival); C57BL/6J (male, 8-12 weeks old, conditioned place preference model)^[1]
Dosage:

50 mg/kg; 100 mg/kg; 250 mg/kg; 150 mg/kg (CPP)
Administration:

i.p.; single dose
Result:

Produced dose-dependent anti-hyperalgesia effect without on-target side effects at therapeutic doses (50 mg/kg, 100 mg/kg) and showed no addiction liability up to 150 mg/kg

Chemical Information

Appearance Solid
Molecular Weight 443.97
Formula C₂₄H₃₀ClN₃O₃
Color Off-white to light yellow
SMILES

O=C(C1=CC2=C(N(C(C3=CC=CC=C3)=O)CC2)C=C1)NCC4(N(C)C)CCOCC4.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cantwell Chater RP, et al. A reversible allosteric inhibitor of GlyT2 alleviates neuropathic pain without on-target side effects. bioRxiv [Preprint]. 2025 Nov 20:2025.04.21.649698.
[Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

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RPI-GLYT2-82

All GlyT Isoforms

All 5-HT Receptor Isoforms