ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).
Aliskiren (CGP 60536) D6 Hydrochloride is a deuterium-labeled Aliskiren. Aliskiren hemifumarate is a direct and orally active renin inhibitor (IC50: 1.5 nM).
Cetirizine D4 dihydrochloride is a deuterium-labeled Cetirizine. Cetirizine is a second-generation antihistamine and a long-acting histamine H1-receptor antagonist.
Hydroxyzine D4 is a deuterium-labeled variation of Hydroxyzine, a chemical compound known for its anticholinergic, anxiolytic, and analgesic properties. It is classified as a heterocyclic histamine H1-receptor antagonist.
Fluvastatin sodium is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.Fluvastatin D6 sodium is deuterium labeled Fluvastatin sodium.
Brexpiprazole S-oxide D8 (DM-3411 D8) is a deuterium-labeled Brexpiprazole S-oxide, the primary metabolite of Brexpiprazole, which is a partial agonist of human 5-HT1A and dopamine receptors (Kis: 0.12 nM and 0.3 nM).
Medroxyprogesterone acetate D3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
Quetiapine D4 fumarate is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a agonist of 5-HT receptors and a antagonist of dopamine receptor,with antidepressant and anxiolytic.
Clomipramine D3 is the deuterium-labeled Clomipramine. Clomipramine is a serotonin transporter, norepinephrine transporter dopamine transporter blocker (Ki: 0.14, 54 and 3 nM).
Bendamustine D4 is the deuterium-labeled Bendamustine. Bendamustine is a DNA cross-linking compound with alkylating and antimetabolite properties. Bendamustine causes DNA breaks.
Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
(S)-(+)-Ibuprofen D3 is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen ,it is an inhibitor of COX-1 and COX-2 activity (IC50s of 2.1 μM and 1.6 μM).
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen is a selective modulator of estrogen receptor (SERM). Tamoxifen is a potent activator of Hsp90 and enhances the Hsp90 molecular chaperone ATPase activity.
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. Etravirine D4 is the deuterium labeled Etravirine.
Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.
Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric aci......
Duloxetine D3 hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).Duloxetine D3 hydrochloride ((S)-Duloxetine D3 hydrochloride) i
Isoproterenol-d7 is intended for use as an internal standard for the quantification of isoproterenol by GC- or LC-MS. Isoproterenol is an agonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 224 and 458 nM, respectively). It is selective for β1- and β2-ARs over β3-ARs (Ki = 1,570 nM). Isoproterenol inhibits contractions in isolated field-stimulated rat vas deferens (EC50 = 45.6 nM). In vivo, isoproterenol (0.33 mg/kg) decreases blood pressure and increases water intake in nephrectomized rats. It reduces blood pressure and increases heart rate in renal hypertensive rabbits. Isoproterenol inhibits histamine-induced bronchospasms in anesthetized dogs. Formulations containing isoproterenol have been used in the treatment of bradydysrhythmias and to improve breathing during anesthesia.
Deutetrabenazine metabolite M4 is believed to be related to its effect as a reversible depletion of monoamines from nerve terminals. The major circulating metabolites of Deutetrabenazine, are reversible inhibitors of VMAT2, resulting in decreased uptake