Aprepitant-13C2, d2 (major)

Aprepitant-13C2, d2 (Major) (MK-0869-13C2, d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.

1217676-37-3

MK-0869-13C2, d2; MK-86-13C2, d2; L-754030-13C2, d2

12352005

Antibiotic; Bacterial; HIV; Isotope-Labeled Compounds; Neurokinin Receptor

Anti-infection; GPCR/G Protein; Neuronal Signaling; Others

Metabolism-protein/nucleotide metabolism

Neurological Disease; Endocrinology; Cancer

O=C1N[13C]([13CH2]N2CCO[C@@H]([C@@H]2C3=CC=C(C=C3)F)O[C@](C[2H])(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)[2H])=NN1

C21 13C2H19D2F7N4O3

538.42

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Martinez AN, et al. Aprepitant limits in vivo neuroinflammatory responses in a rhesus model of Lyme neuroborreliosis. J Neuroinflammation. 2017 Feb 15;14 (1) :37.|[3]Bayati S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016 Nov 15;791:274-283.|[4]Mannangatti P, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl) . 2017 Feb;234 (4) :695-705.|[5]Barrett JS, et al. Pharmacologic rationale for the NK1R antagonist, aprepitant as adjunctive therapy in HIV. J Transl Med. 2016 May 26;14 (1) :148.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W777166/

Isotope-Labeled Compounds

No Development Reported