Fig. 1 · Structure
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GSK256471
NK3 Receptor Antagonist
GSK256471 is a non-peptide antagonist targeting the tachykinin NK3 receptor, exhibiting a pKi of 8.9 for the human recombinant receptor and 8.4 for the guinea pig native receptor. This compound demonstrates over 100-fold selectivity against NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 irreversibly inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and has been shown to mitigate wet dog shaking behavior and suppress dopamine release. This compound serves as a valuable tool for studying the pathophysiology of schizophrenia.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Antagonist |
| CAS Number | 1133706-08-7 |
| Applications | NK3 Receptor Antagonist |
| Formula | C29H29N3O3S |
| Molecular Weight | 499.62 |
| SMILES | O=C(N[C@H](C1=CC=CC=C1)C2CC2)C3=C(C(C4=CC=CC=C4)=NC5=CC=CC=C35)CN(S(=O)(C)=O)C |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.