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GR 159897

CAT: 0804-HY-107691Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-107691Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2) -CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects[1][2].
CAS Number
158848-32-9
UNSPSC
12352005
Target
Neurokinin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Cancer; Endocrinology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/gr-159897.html
Purity
99.60
Solubility
DMSO : 31 mg/mL (ultrasonic; warming)
Smiles
O=[S@](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4
Molecular Formula
C23H27FN2O2S
Molecular Weight
414.54
References & Citations
[1]Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272 (2-3) :241-8.|[2]Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NK2R