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(R)-Nepicastat hydrochloride

Cat. No. M2349
(R)-Nepicastat hydrochloride Structure
Synonym:

RS-25560-198 HCl

Size Price Availability
10mg USD 198  USD220 Out of stock
50mg USD 495  USD550 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Nepicastat is a novel inhibitor of dopamine-beta-hydroxylase, the enzyme which catalyses the conversion of dopamine to noradrenaline in sympathetic nerves. (R)-Nepicastat (30 mg/kg, p.o.) reduces noradrenaline content, dopamine content and dopamine/noradrenaline ratio in mesenteric artery and left ventricle of spontaneously hypertensive rats (SHRs).

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 331.81
Formula C14H15F2N3S.HCl
CAS Number 195881-94-8
Purity >98%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.
Stanley WC, et al. Br J Pharmacol. 1997 Aug;121(8):1803-1809. PMID: 9283721.

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Keywords: (R)-Nepicastat hydrochloride, RS-25560-198 HCl supplier, HCV Protease, inhibitors

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