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(R)-Nepicastat hydrochloride

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

RS-25560-198 HCl

Size Price Availability
10mg USD 220  USD220 Out of stock
50mg USD 550  USD550 Out of stock
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Quality Control & Documentation
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).

Chemical Information
Molecular Weight 331.81
Formula C14H15F2N3S.HCl
CAS Number 195881-94-8
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Stanley WC, et al. Br J Pharmacol. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.

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


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