NETUPITANT

NETUPITANT

Biochem/physiol Actions

Netupitant is a brain-penetrant, orally active, potent and selective neurokinin-1 (NK1) receptor (NK1R; Tachykinin receptor 1) antagonist (Ca+2 mobilization IC50 = 11.2 nM/hNK1 vs. >1 µM/rNK1 & hNK2/3; hNK1/2/3 Ki = 0.95 nM/1.6 µM/1.6 µM) that effectively blocks agonist GR73632-induced foot tapping in gerbils (ID50 = 0.5 mg/kg po 2h prior to 3 pmol/5 µL GR73632/gerbil icv). In addition to antiemetic efficacy against substance P-associated vomiting reflexes, netupitant is also reported to enhance the analgesic effects of electroacupuncture (EA) among humanized mice with sickle cell disease in response to pain in vivo (10 mg/kg/day, i.p.).

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576741 NETUPITANT white to beige 100 SIGMA-ALDRICH 2-8°C
£120.34 (exc VAT) per EACH
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3576742 NETUPITANT white to beige 100 SIGMA-ALDRICH 2-8°C
£487.50 (exc VAT) per EACH
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