Rolapitant

• Description :

  Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model[1][2].

• Product Name Alternative :

  SCH619734

• UNSPSC :

  12352005

• Hazard Statement :

  H315, H319, H320

• Target :

  Neurokinin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; Neuronal Signaling

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/Rolapitant.html

• Purity :

  99.89

• Solubility :

  DMSO : ≥ 30 mg/mL

• Smiles :

  C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)OC[C@@]2(C3=CC=CC=C3)CC[C@@]4(NC(CC4)=O)CN2

• Molecular Formula :

  C25H26F6N2O2

• Molecular Weight :

  500.48

• Precautions :

  H315, H319, H320

• References & Citations :

  [1]Duffy RA, et al. Rolapitant (SCH 619734) : a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102 (1) :95-100.|[2]Rapoport B, et al. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC) . Support Care Cancer. 2015 Nov;23 (11) :3281-8.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  NK1R

• CAS Number :

  [552292-08-7]