(Rac)-Monepantel-d₅ 

(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

478.42

C₂₀H₈D₅F₆N₃O₂S

2747918-33-6

887148-69-8

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Hess J, et al. Assessment of the nematocidal activity of metallocenyl analogues of monepantel. Dalton Trans. 2016 Nov 28;45(44):17662-17671  [Content Brief]

  [3]. Bahrami F, et al. Monepantel induces autophagy in human ovarian cancer cells through disruption of the mTOR/p70S6K signalling pathway. Am J Cancer Res. 2014 Sep 6;4(5):558-71.  [Content Brief]

  [4]. Raza A, et al. Increased expression of ATP binding cassette transporter genes following exposure of Haemonchus contortus larvae to a high concentration of monepantel in vitro. Parasit Vectors. 2016 Sep 29;9(1):522.  [Content Brief]

  [5]. Stuchlikova, et al. Monepantel induces hepatic cytochromes p450 in sheep in vitro and in vivo. Chem Biol Interact. 2015 Feb 5;227:63-8. ?  [Content Brief]