Product Name :
GR 159897
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.
CAS:
158848-32-9
Molecular Weight:
414.54
Formula:
C23H27FN2O2S
Chemical Name:
3-(2-4-[(benzenesulfinyl)methyl]-4-methoxypiperidin-1-ylethyl)-5-fluoro-1H-indole
Smiles :
COC1(CS(=O)C2C=CC=CC=2)CCN(CCC2=CNC3=CC=C(F)C=C23)CC1
InChiKey:
BANYJBHWTOJQDU-UHFFFAOYSA-N
InChi :
InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 158848-32-9|Molecular Weight: 414.54|Formula: C23H27FN2O2S|Chemical Name: 3-(2-4-[(benzenesulfinyl)methyl]-4-methoxypiperidin-1-ylethyl)-5-fluoro-1H-indole|Smiles: COC1(CS(=O)C2C=CC=CC=2)CCN(CCC2=CNC3=CC=C(F)C=C23)CC1|InChiKey: BANYJBHWTOJQDU-UHFFFAOYSA-N|InChi: InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Glatiramer Epigenetic Reader Domain |Shelf Life: ≥12 months if stored properly.Topiramate Biological Activity |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:32809584 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells. GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM and 4T1 cells) treatment increases phosphorylation of P38, while inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM and 4THM but not in 4T1 cells.|In Vivo:|GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h).|Products are for research use only. Not for human use.|
