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SCH 619734

Cat. No. M9019
SCH 619734 Structure
Synonym:

Rolapitant

Size Price Availability Quantity
5mg USD 135  USD150 In stock
10mg USD 207  USD230 In stock
25mg USD 414  USD460 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SCH-619734 is an orally bioavailable, centrally-acting, selective neurokinin 1 receptor (NK1-receptor) antagonist with a Ki of 0.66 nM. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 500.48
Formula C25H26F6N2O2
CAS Number 552292-08-7
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy.
Rapoport B, et al. Eur J Cancer. 2016 Apr;57:23-30. PMID: 26851398.

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).
Rapoport B, et al. Support Care Cancer. 2015 Nov;23(11):3281-8. PMID: 25940030.

Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.
Duffy RA, et al. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. PMID: 22497992.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SCH 619734, Rolapitant supplier, Neurokinin Receptor, inhibitors

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