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Thiorphan

Cat. No. M20002
Thiorphan  Structure
Synonym:

Neprilysin/neutral endopeptidase inhibitor

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 95  USD95 In stock
25mg USD 185  USD185 In stock
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Quality Control & Documentation
Biological Activity

Thiorphan was a selective neprilysin inhibitor with an IC50 value of 6.9 nM. Increased bradykinin-induced relaxation of isolated porcine coronary rings with potassium chloride precontraction under hypoxic but very oxygen conditions.

Chemical Information
Molecular Weight 253.32
Formula C12H15NO3S
CAS Number 76721-89-6
Solubility (25°C) Ethanol: 50 mg/mL
DMSO: 30 mg/mL
Storage -20°C
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] Shaunivan L Labiuk, et al. Acta Crystallogr F Struct Biol Commun. Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan

[2] Marion Eberlin, et al. BMC Pediatr. Racecadotril in the treatment of acute diarrhea in children: a systematic, comprehensive review and meta-analysis of randomized controlled trials

[3] Christopher Stewart Heather. BMJ Clin Evid. Travellers' diarrhoea

[4] R Greenberg, et al. Life Sci. Thiorphan potentiation of stress-induced analgesia in the mouse

[5] M Chicau-Chovet, et al. Eur J Pharmacol. Thiorphan and acetorphan inhibit gastric secretion by a central, non-opioid mechanism in the rat

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  Catalog
Abmole Inhibitor Catalog




Keywords: Thiorphan , Neprilysin/neutral endopeptidase inhibitor supplier, Neprilysin (NEP), inhibitors, activators


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