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(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
Debutyldronedarone-d6 (hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent[1][2].
Trimethobenzamide-d6 is deuterium labeled Trimethobenzamide. Trimethobenzamide is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
Iclaprim-d6 (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
Nilutamide-d6 (Nilandron-d6) is the deuterium labeled Nilutamide. Nilutamide (Nilandron) is a non-steroidal anti-androgen agent proposed in the research of metastatic prostatic carcinoma[1][2].
Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
Olmesartan medoxomil-d6 (CS 866-d6) is the deuterium labeled Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM[1][2].
8-Chlorotheophylline-d6(8-Chlorotheophylline-d6) is the deuterium-labeled 8-Chlorotheophylline (HY-W014203) . 8-Chlorotheophylline is an organic compound.
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Erlotinib-d6 (hydrochloride) a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM[1]. Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bensulfuron-methyl-d6 is a deuterated Bensulfuron-methyl (HY-B0870) (sulfonylurea pesticides). Bensulfuron-methyl-d6 can be used as an internal standard for the determination of pesticide residues by LC-MS[1].
Cipepofol-d6(Ciprofol-d6;HSK3486-d6) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
Norgestrel-d6 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives. Norgestrel-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mavacamten-d6(MYK461-d6;SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Olmesartan-d6(RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure[1][2].
N-Acetyl Norgestimate-d6 is the deuterium labeled N-Acetyl Norgestimate[1]. N-Acetyl Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
Cipepofol-d6-2(Ciprofol-d6-2;HSK3486-d6-2) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Ternidazole-d6 (hydrochloride) is the deuterium labeled Ternidazole hydrochloride. Ternidazole hydrochloride is a hydroxymetabolite of nitroimidazole, has antiprotozoic properties[1][2].
Eldecalcitol-d6 is the deuterium labeled Eldecalcitol. Eldecalcitol is an orally active analogue of active vitamin D used in the treatment of osteoporosis.
rel-Ritonavir-d6 (rel-ABT 538-d6;rel-RTV-d6) is the deuterium labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Norgestimate-d6 is the deuterium labeled Norgestimate. Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive[1][2]. Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Aminoadipic acid-d6 is deuterated labeled Aminoadipic acid (HY-113328). Aminoadipic acid is an intermediate in the metabolism of lysine and glycopurine.
Ciprofibrate-d6 is deuterium labeled Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha[1].
Podofilox-d6 is the deuterium labeled Podofilox. Podofilox (Podophyllotoxin) is a potent inhibitor of microtubule assembly and DNA topoisomerase II[1][2].
Fenofibric acid-d6 (FNF acid-d6) is the deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
Enasidenib-d6(AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
Ivabradine-d6 (hydrochloride) is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
Dydrogesterone-d6 is the deuterium labeled Dydrogesterone. Dydrogesterone is a potent, orally active progestogen indicated in a wide variety of gynaecological conditions related to progesterone deficiency.
Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
4',7-Dimethoxyisoflavone-d6(Dimethoxydaidzein-d6) is the deuterium labeled 4',7-Dimethoxyisoflavone (HY-N2145). 4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity .
Tetracycline-d6 is the deuterium labeled Tetracycline. Tetracycline is a broad-spectrum antibiotic, exhibiting activity against a wide range of gram-positive and gram-negative bacteria.
Paraxanthine-d6 is the deuterium labeled Paraxanthine. Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.
Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
Picropodophyllin-d6(AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Elacestrant-d6(RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
Acamprosate-d6 (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems[1].
Bilastine-d6 is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria[1][2].
Irbesartan-d6 is the deuterium labeled Irbesartan. Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
Norethindrone-d6 is the deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea. Norethindrone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propionylpromazine-d6 (hydrochloride) is the deuterium labeled Propionylpromazine hydrochloride. Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease[1].
Rifaximin-d6 is the deuterium labeled Rifaximin. Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity[1][2].
Tetrahydrocortisone-d6 is the deuterium labeled Tetrahydrocortisone. Tetrahydrocortisone is a stress-induced hormone. Tetrahydrocortisone is also a urinary metabolite of Cortisone derived from the reduction of Cortisone by 5-reductase[1].
Piperaquine-d6 is the deuterium labeled Piperaquine[1]. Piperaquine is a bisquinoline antimalarial agent. Piperaquine can be used in antimalarial research in combination with Artemisinin[2][3].
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone[1]. 22-Hydroxy Mifepristone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Syringic acid-d6 is the deuterium labeled Syringic acid[1]. Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation[2][3].
Paricalcitol-d6 is the deuterium labeled Paricalcitol. Paricalcitol is a agent used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure[1].
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Maribavir-d6(1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[1][2].
(Rac)-Tenofovir-d6 is a labelled racemic Tenofovir. Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
L-Ornithine-d6 (hydrochloride) is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
Chlorotoluron-d6 is the deuterium labeled Chlorotoluron[1]. Chlorotoluron (Chlortoluron) is a substituted phenylurea herbicide, is widely used for selective weed control in cereals crops and is an environmental pollutant[2].
Piperaquine-d6 (tetraphosphate) is the deuterium labeled Piperaquine tetraphosphate. Piperaquine tetraphosphate is a bisquinoline antimalarial agent. Piperaquine phosphate can be used in antimalarial research in combination with Artemisinin[1][2].
Dobesilate-d6 (calcium) is deuterium labeled Calcium dobesilate. Calcium dobesilate, a vasoprotective, is widely used in chronic venous disease, diabetic retinopathy and the symptoms of haemorrhoidal attack in many countries.
Venlafaxine-d6 is the deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Flunisolide-d6 is the deuterium labeled Flunisolide. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
3,4-Dimethoxy-benzaldehyde-d6 is the deuterium labeled Veratraldehyde[1]. Veratraldehyde is an important chemical used in perfumery, agrochemical, and pharmaceutical industries.
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Choline-d6 (chloride) is the deuterium labeled Choline chloride. Choline chloride is an organic compound and a quaternary ammonium salt, an acyl group acceptor and choline acetyltransferase substrate, also is an important additive in feed especially for chickens where it accelerates growth.
Lanosterol-d6 is deuterium labeled Lanosterol. Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol s
Captan-d6 is the deuterium labeled Captan[1]. Captan is a common agricultural fungicide used to control Botrytis, Fusarium, Fusicoccum, Pythium. Captan enhances denitrifying and total culturable bacteria[2].
Rizatriptan-d6 (benzoate) is the deuterium labeled Rizatriptan benzoate. Rizatriptan benzoate is a 5-HT1 agonist triptan agent for the treatment of migraine headaches[1][2].
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
25-Hydroxycholesterol-d6(25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells[1][2].
Desmosterol-d6 is the deuterium labeled Desmosterol. Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism[1].
Pirimicarb-d6 is the deuterium labeled Diuron. Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male
Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
L-Citrulline-d6 is the deuterium labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea[1][2].
Baquiloprim-d6 is deuterium labeled Baquiloprim. Baquiloprim, an antibiotic, is a selective inhibitor of bacterial dihydrofolate reductases. Baquiloprim possesses in vitro bacteriostatic activity against both Gram-negative and Gram-positive bacteria[1][2].
Dapoxetine-d6 is the deuterium labeled Dapoxetine[1]. Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE)[2].
2-Methylpyrazine-d6 is the deuterium labeled 2-Methylpyrazine[1]. 2-Methylpyrazine is a kind of alkylpyrazine that can be identified in roasted red pepper seed oils[2].
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Verapamil-d6(CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
1,3-Propanediol-d6 is the deuterium labeled 1,3-Propanediol[1]. 1,3-Propanediol is produced in nature by the fermentation of glycerol in microorganism[2].
Methylprednisolone acetate-d6 is the deuterium labeled Methylprednisolone acetate (HY-13681). Methylprednisolone acetate, a prednisolone derivative, is a corticosteroid hormone. Methylprednisolone acetate can relieve pain and swelling that occurs with arthritis and other joint disorders in vivo .
l-α-tocopherol acetate- 13C4,d6 is the 13C- and deuterium-labeled l-α-tocopherol acetate. l-α-tocopherol acetate is a natural tocopherol and has potent antioxidant activities[1].
Dansyl-2-(2-azidoethoxy)ethanamine-d6 is the deuterium labeled Dansyl-2-(2-azidoethoxy)ethanamine[1]. Dansyl-2-(2-azidoethoxy)ethanamine-d6 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Esomeprazole-d6 sodium is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte[1].
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
Hexazinone-d6 is the deuterium labeled Hexazinone[1]. Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis[2].
Leucocrystal violet-d6 is the deuterium labeled Leucocrystal violet[1]. Leucocrystal violet is a triphenylmethane dye which can be used to detect antimony in environmental and biological samples using spectrophotometric techniques[2][3].
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
Isoxsuprine-d6 (hydrochloride) is the deuterium labeled Isoxsuprine hydrochloride. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
Diltiazem-d6 is the deuterium labeled Diltiazem. Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
α-Tocopherol-d6 (acetate) is the deuterium labeled D-α-Tocopherol acetate. D-α-Tocopherol acetate (D-Vitamin E acetate) can be hydrolyzed to d-alpha-tocopherol (VE) and absorbed in the small intestine[1].
Dehydroepiandrosterone sulfate-d6 (sodium dihydrate) is the deuterium labeled tert-Butyl N-[(1S)-1-[Methoxy(methyl)carbamoyl]-2-phenylethyl]carbamate[1].
Glutaric acid-d6 is the deuterium labeled Glutaric acid. Glutaric acid is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
4-Methylcatechol-d6 is the deuterium labeled 4-Methylcatechol[1]. 4-Methylcatechol, a metabolite of p-toluate, is a substrate as well as a suicide inhibitor of Catechol 2,3-Dioxygenase[2].
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Dimethyl fumarate-d6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression[1][2][3][4][5][6].
Risdiplam-hydroxylate-d6 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels .
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Metolachlor-d6 is the deuterium labeled Metolachlor[1]. Metolachlor is a pre-emergent selective, chloroacetanilide herbicide for the control of a variety of annual grass and broad leaf weeds in corn and other crops. Metolachlor is a chiral herbicide consisting of four stereoisomers[2][3].
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
H-Abu-OH-d6 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
Melitracen-d6 (hydrochloride) is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space[1][2].
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].
Nicosulfuron-d6 is the deuterium labeled Nicosulfuron[1]. Nicosulfuron is a selective herbicide belonging to the sulfonylurea family. Nicosulfuron is commonly used as a post-emergence herbicide to protect maize crops from weeds. Nicosulfuron inhibits acetolactate synthase (ALS) enzyme activity[2].
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins[1].
Alendronic acid-d6 is the deuterium labeled Alendronic acid. Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease[1].
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
D-Ribose-d6 is the deuterium labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein gl
Methyl syringate-d6 is the deuterium labeled Methyl syringate[1]. Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist[2][3][4].
2-Methylsuccinic acid-d6 is the deuterium labeled 2-Methylsuccinic acid[1]. 2-Methylsuccinic acid is a normal metabolite in human fluids and the main biochemical measurable features in ethylmalonic encephalopathy[2][3].
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Metoprolol-d6 (tartrate) is the deuterium labeled Metoprolol tartrate. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3][4].
4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds[1][2].
Chlorprothixene-d6 (hydrochloride) is the deuterium labeled Chlorprothixene hydrochloride. Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
Metalaxyl-d6 is the deuterium labeled Metalaxyl. Metalaxyl is a fungicide that inhibits protein synthesis in fungi. Metalaxyl inhibits the growth of potato blight (P. infestans) fungal isolates from Serbian potato fields (EC50s=0.3-3.9 μg/mL).
Trandolaprilate-d6 is the deuterium labeled Trandolaprilate[1]. Trandolaprilate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity[2][3].
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
3-Mercapto-3-methylbutan-1-ol-d6 is the deuterium labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Dimethoate-d6 is the deuterium labeled Dimethoate. Dimethoate is an effective systemic insecticide for use on plants, has shown promise as a chemotherapeutic agent for control of cattle grubs and certain other insect pests of farm animals, and has high contact toxicity to house-flies and many other insects[1].
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification[1][2].
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit[1]. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis[2].
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
DL-Norepinephrine-d6 (hydrochloride) is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension[1].
4-Epitetracycline-d6 is deuterated labeled 4-Epitetracycline hydrochloride (HY-136443) 4-Epitetracycline hydrochloride is an epimer of Tetracycline (HY-A0107). Tetracycline can undergo epimerization insolution to 4-Epitetracycline hydrochloride, which shows a much lower antibiotic activity.
Calcifediol-d6 (monohydrate) is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), a major circulating metabolite of vitamin D3, is a potent VDR ligand .
1,3-Dimethoxybenzene-d6 is the deuterium labeled 1,3-Dimethoxybenzene[1]. 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds[2].
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone[1]. 1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity[2].
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Propane-1,2,3-triyl tripalmitate-d6 is the deuterium labeled Propane-1,2,3-triyl tripalmitate. Propane-1,2,3-triyl tripalmitate is an endogenous metabolite.
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
DL-dithiothreitol-d6 is the deuterium labeled DL-dithiothreitol[1]. DL-dithiothreitol (DTT) is a reducing agent. DL-dithiothreitol forms a stable six-membered ring with an internal disulfide bond once oxidized[2].
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
Ranitidine-d6 (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].
Enterolactone-d6 is the deuterium labeled Enterolactone. Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity[1]. Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis[2].
Erythromycin-d6 is the deuterium labeled Erythromycin. Erythromycin is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Fenitrothion-d6 is the deuterium labeled Fenitrothion[1]. Fenitrothion, one of the most widely used organophosphorus pesticides, is a cholinesterase inhibiting insecticide/acaricid. Fenitrothion is widely used, as a broad-spectrum insecticide, on cotton crops, vegetables crops, fruit crops, and field crops especially paddy. Fenitrothion leads to accumulation of nitrophenols[2][3].
Pirimiphos-methyl-d6 is the deuterium labeled Pirimiphos-methyl. Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains[1][2][3].
Metalaxyl-M-d6 is the deuterium labeled Metalaxyl-M[1]. Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division[2].
(Rac)-Zearalenone-d6 is the deuterium labled Zearalenone (HY-103447). Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D[1][2].
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
Diacerein-d6 is the deuterium labeled Diacerein[1]. Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases[2].
Bezafibrate-d6 is the deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Dihomo-γ-linolenic acid-d6(DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
Antimalarial agent 11 (compound 1), a spirocyclic chromane, is a potent antimalarial agent. Antimalarial agent 11 exhibits excellent potency with an EC50 of 350 nM against the Chloroquine-resistant Dd2 strain. Antimalarial agent 11 has EC50s of 1.48 µM and 1.81 µM against D6 and ARC08-022 strains, respectively .
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
1-(4-Hydroxyphenyl)-2-((4-(4-hydroxyphenyl)butan-2-yl)amino)ethanone-d6 (hydrochloride) is the deuterium labeled 1-(4-Hydroxyphenyl)-2-((4-(4-hydroxyphenyl)butan-2-yl)amino)ethanone hydrochloride[1].
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities[1][2].
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
5-Hydroxyindole-3-acetic acid-d6 is the deuterium labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].
Toremifene-d6 (citrate) is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Canagliflozin-d6 is the deuterium labeled Canagliflozin[1]. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[2].
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity[1][2].
Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].
Buprofezin-d6 is the deuterium labeled Buprofezin. Buprofezin is a broad-spectrum insecticide and chitin synthesis inhibitor that targets developmental stage coleopteran pests.Buprofezin promotes the conversion of energy metabolism from the aerobic tricarboxylic acid (TCA) cycle and oxidative phosphorylation to anaerobic glycolysis. Buprofezin also promotes the production of reactive oxygen species (ROS) by inhibiting cytochrome c oxidase[1][2].
Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
Tricin-d6 is the deuterium labeled Tricin[1]. Tricin is a natural flavonoid present in large amounts in Triticum aestivum. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7[2][3][4].
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Ribociclib-d6 is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Ribociclib-d6 (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Umifenovir-d6 (hydrochloride) is the deuterium labeled Umifenovir hydrochloride. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity[3].
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Bisphenol A-d6 is the deuterium labeled Bisphenol A. Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders[1][2][3].
Squalene-d6 is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis[1][2][3][4][5].
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
Melengestrol acetate-d6 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate[1]. DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition[2][3].
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
(7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is the deuterium labeled MCA[1]. MCA is a coumarin derivative. MCA quantitates platelet-activating factor by high-performance liquid chromatography with fluorescent detection. MCA can modify FRET peptide substrates for analyzing protease activities[2][3]. (7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system[1].
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87[1][2].
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance[1][2].
Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
Irbesartan-d6-1 is the deuterium labeled Irbesartan[1]. Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease[2].
Sucralose-d6 is deuterium labeled Sucralose. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents[1][2].
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride[1]. Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2][3][4][5][6][7].
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
N-Hydroxy (E)-2-(4-methoxybenzoxy)-4-methoxy-3-prenylcinnamamide-d6 is the deuterium labeled N-Hydroxy (E)-2-(4-methoxybenzoxy)-4-methoxy-3-prenylcinnamamide[1].
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
(rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1][2].
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
N1-Acetylspermidine-d6 (hydrochloride) is the deuterium labeled N1-Acetylspermidine hydrochloride. N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA[1][2][3].
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine[1]. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[2].
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome[1][2].
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
Dalbavancin-d6 is the deuterium labeled Dalbavancin[1]. Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[2][3].
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects[1][2][3].
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol[1]. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents[2].
Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
5α-Cholesta-7,24-dien-3β-ol-d6 is deuterium labeled 5α-Cholesta-7,24-dien-3β-ol. 5α-Cholesta-7,24-dien-3β-ol, a sterol, can be found in hamster cauda epididymal mature spermatozoa[1].
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels[1].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment .
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
(rac)-Dobutamine-d6 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
Nitidanin ((±)-Nitidanin) is an antimalarial and antiviral compound that can be isolated from the wood of Xanthoxylum nitidun D. C. Nitidanin is shows IC50 values of 21.2 and 18.4 μM for D6 and W2 clones of Plasmodium falciparum, respectively. Nitidanin can be used for the research of malaria and virus infection .
SARS-CoV-2 3CLpro-IN-21 (Compound D6) irreversibly and covalently inhibits SARS-CoV-2 3CL pro with an IC50 of 0.03 μM. SARS-CoV-2 3CLpro-IN-21 also inhibits SARS-CoV-13CL pro with an IC50 of 0.12μM .
Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway .
DMABA NHS ester can chemically react with the primary amine groups of the major phospholipid component of the cell membrane, Phosphatidylethanolamine (PE). Through precursor ion scanning, all PE subclasses labeled with DMABA can be detected. DMABA NHS ester can be used in combination with isotope-labeled compounds such as DMABA-d6 NHS ester, DMABA-d10 NHS ester, and DMABA-d4 NHS ester to observe changes in the distribution of PE lipids and the formation of novel PE lipid products .
CYP2D6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside, an anthraquinone glucoside, can be isolated from Rheum undulatum L. Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside has potent DPPH radical and ?O2- scavenging activity .
(Rac)-Bedaquiline-d6is the deuterium labeledBedaquiline(HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
3-epi-25-Hydroxy Vitamin D3-d6is the deuterium labeled3-epi-25-Hydroxy Vitamin D3(HY-142140) . 3-epi-25-Hydroxy Vitamin D3 is the vitamin D metabolite, while vitamin D metabolism highly dependent on macrophage polarization. The C3-epimerase pathway for vitamin D is active in macrophages .
2′-β-C-Methyl-beta-D-6-methylpurine riboside is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
Maxacalcitol-d66 is the deuterated form of Maxacalcitol (22-Oxacalcitriol), which is a non-calcemic vitamin D3 analog and VDR ligand of VDR-like receptors.
Quercetin 3-O-β-D-(6''-p-coumaroyl)glucopyranosyl(1→2)-α-L-rhamnopyranoside (Quercetin-3-O-[2-O-(6-O-p-hydroxyl-E-coumaroyl)-D-glucosyl]-(1→2)-L-rhamnoside) is one of the major antioxidants of Ginkgo biloba leaves .
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity .
Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM .
4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties .
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM) .
Antihistamine-1 is a H1-antihistamine(Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2 .
IN-2-LF is an inhibitor of lethal factor. IN-2-LF also inhibits furin with an IC50 of 2 μM. IN-2-LF enhances protection against anthrax lethal toxin when in combination with D6R .
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .
CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
Thermopsoside is a flavone derivative isolated from Aspalathus linearis. Thermopsoside exhibits inhibitory effects on CYP450 isozymes with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM, 32.0 μM, for CYP3A4, CYP2C19, CYP2D6 and CYP2C9, respectively .
Anticancer agent 127 (142D6) is an IAP inhibitor that covalently targets the BIR3 domains of XIAP, cIAP1, and cIAP2. Anticancer agent 127 targets the BIR3 domains of XIAP, cIAP1, and cIAP2 with IC50s of 12 nM, 14 nM, and 9 nM, respectively. Anticancer agent 127 has anticancer effects .
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment .
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice .
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
IN-2-LF is an inhibitor of lethal factor. IN-2-LF also inhibits furin with an IC50 of 2 μM. IN-2-LF enhances protection against anthrax lethal toxin when in combination with D6R .
Quercetin 3-O-β-D-(6''-p-coumaroyl)glucopyranosyl(1→2)-α-L-rhamnopyranoside (Quercetin-3-O-[2-O-(6-O-p-hydroxyl-E-coumaroyl)-D-glucosyl]-(1→2)-L-rhamnoside) is one of the major antioxidants of Ginkgo biloba leaves .
Nitidanin ((±)-Nitidanin) is an antimalarial and antiviral compound that can be isolated from the wood of Xanthoxylum nitidun D. C. Nitidanin is shows IC50 values of 21.2 and 18.4 μM for D6 and W2 clones of Plasmodium falciparum, respectively. Nitidanin can be used for the research of malaria and virus infection .
Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside, an anthraquinone glucoside, can be isolated from Rheum undulatum L. Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside has potent DPPH radical and ?O2- scavenging activity .
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
Thermopsoside is a flavone derivative isolated from Aspalathus linearis. Thermopsoside exhibits inhibitory effects on CYP450 isozymes with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM, 32.0 μM, for CYP3A4, CYP2C19, CYP2D6 and CYP2C9, respectively .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
ACKR2 Protein, an atypical chemokine receptor, controls chemokine levels and localization with high-affinity binding. Operating independently, ACKR2, also known as an interceptor or decoy receptor, interacts with diverse chemokines, triggering a beta-arrestin 1-dependent signaling pathway. This pathway facilitates ACKR2 relocation, enhancing efficiency in chemokine uptake and degradation. Scavenging chemokines in various tissues, ACKR2 plays a pivotal role in resolving inflammation, regulating adaptive immune responses, and influencing leukocyte interactions with lymphatic endothelial cells. ACKR2 contributes significantly to immune silencing of macrophages during inflammation resolution. ACKR2 Protein, Human (Cell-Free, His) is the recombinant human-derived ACKR2 protein, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of ACKR2 Protein, Human (Cell-Free, His) is 384 a.a., with molecular weight of 46.9 kDa.
LRIG1 protein serves as a feedback negative regulator in receptor tyrosine kinase signaling, enhancing receptor ubiquitination and facilitating intracellular degradation. It interacts with various receptors, including EGFR/ERBB1, ERBB2, ERBB3, and ERBB4, through its extracellular leucine-rich repeat (LRR) and immunoglobulin-like domains. The physiological relevance of these interactions is debated, as LRIG1 may have low EGFR affinity, requiring elevated LRIG1 and receptor kinase levels for interaction. LRIG1 Protein, Human (HEK293, His) is the recombinant human-derived LRIG1 protein, expressed by HEK293, with C-His labeled tag. The total length of LRIG1 Protein, Human (HEK293, His) is 745 a.a., with molecular weight of 85-105 kDa.
The LRIG1 protein acts as a feedback negative regulator of receptor tyrosine kinase signaling, enhancing receptor ubiquitination and promoting intracellular degradation. It interacts with various receptors, including EGFR/ERBB1, ERBB2, ERBB3, and ERBB4, through its extracellular leucine-rich repeats (LRR) and immunoglobulin-like domains. LRIG1 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived LRIG1 protein, expressed by HEK293 , with C-His labeled tag. The total length of LRIG1 Protein, Cynomolgus (HEK293, His) is 759 a.a., with molecular weight of 90-110 kDa.
The DDX39B protein intricately coordinates nuclear mRNA export and is specifically associated with spliced mRNA as a key component of the TREX complex. This coupling of mRNA transcription, processing, and export involves rounds of ATP-dependent hydrolysis, recruiting components such as ALYREF/THOC and CHTOP. DDX39B Protein, Human (GST) is the recombinant human-derived DDX39B protein, expressed by E. coli , with N-GST labeled tag. The total length of DDX39B Protein, Human (GST) is 250 a.a., with molecular weight of ~55.2 kDa.
The TCblR/CD320 protein is a receptor for cobalamin-saturated transcobalamin (TCbl) and is critical for cobalamin uptake and can influence cell physiology. At the plasma membrane, it is expressed on follicular dendritic cells (FDC), where it helps interact with germinal center B cells and promotes immune responses. TCblR/CD320 Protein, Rat (HEK293, Fc) is the recombinant rat-derived TCblR/CD320 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of TCblR/CD320 Protein, Rat (HEK293, Fc) is 182 a.a., with molecular weight of ~47.3 KDa.
The CYP2D6 protein, a vital cytochrome P450 monooxygenase, metabolizes diverse substrates, including fatty acids and steroids. It catalyzes epoxidation, hydroxylation, and oxidative conversion, impacting endocannabinoid signaling, cholesterol homeostasis, and drug metabolism, highlighting its multifunctional role in cellular processes. CYP2D6 Protein, Human is the recombinant human-derived CYP2D6 protein, expressed by E. coli , with tag free. The total length of CYP2D6 Protein, Human is 464 a.a., .
The CYP2D6 protein, a vital cytochrome P450 monooxygenase, metabolizes diverse substrates, including fatty acids and steroids. It catalyzes epoxidation, hydroxylation, and oxidative conversion, impacting endocannabinoid signaling, cholesterol homeostasis, and drug metabolism, highlighting its multifunctional role in cellular processes. CYP2D6 Protein, Human (His) is the recombinant human-derived CYP2D6 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CYP2D6 Protein, Human (His) is 464 a.a., .
TCblR/CD320 is the receptor for cobalamin (TCbl) and is critical for cellular cobalamin homeostasis and B cell responses. It is expressed on follicular dendritic cells, interacts with germinal center B cells, and coordinates immune responses. TCblR/CD320 Protein, Human (HEK293, His) is the recombinant human-derived TCblR/CD320 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of TCblR/CD320 Protein, Human (HEK293, His) is 196 a.a., with molecular weight of 37-53 kDa.
TCblR/CD320 Protein, the receptor for cobalamin-saturated transcobalamin (TCbl), plays a pivotal role in cobalamin uptake, expressed on the plasma membrane and notably on follicular dendritic cells (FDC). As a costimulator, TCblR promotes B cell responses, fostering differentiation and proliferation. It's particularly influential in differentiating germinal center-B cells, engaging in collaborative interactions with T-cells and FDC. CD320 enhances IL-10-induced precursor proliferation, underscoring its significance in cobalamin homeostasis and cellular processes through interactions with TCN2. TCblR/CD320 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived TCblR/CD320 protein, expressed by HEK293, with C-hFc labeled tag. The total length of TCblR/CD320 Protein, Mouse (HEK293, Fc) is 208 a.a., with molecular weight of ~72.5 kDa.
TCblR/CD320 Protein, the receptor for cobalamin-saturated transcobalamin (TCbl), plays a pivotal role in cobalamin uptake, expressed on the plasma membrane and notably on follicular dendritic cells (FDC). As a costimulator, TCblR promotes B cell responses, fostering differentiation and proliferation. It's particularly influential in differentiating germinal center-B cells, engaging in collaborative interactions with T-cells and FDC. CD320 enhances IL-10-induced precursor proliferation, underscoring its significance in cobalamin homeostasis and cellular processes through interactions with TCN2. TCblR/CD320 Protein, Mouse (HEK293, His) is the recombinant mouse-derived TCblR/CD320 protein, expressed by HEK293, with C-His labeled tag. The total length of TCblR/CD320 Protein, Mouse (HEK293, His) is 208 a.a., with molecular weight of ~47.7 kDa.
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
Trimethobenzamide-d6 is deuterium labeled Trimethobenzamide. Trimethobenzamide is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
Iclaprim-d6 (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
Nilutamide-d6 (Nilandron-d6) is the deuterium labeled Nilutamide. Nilutamide (Nilandron) is a non-steroidal anti-androgen agent proposed in the research of metastatic prostatic carcinoma[1][2].
Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
Olmesartan medoxomil-d6 (CS 866-d6) is the deuterium labeled Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM[1][2].
8-Chlorotheophylline-d6(8-Chlorotheophylline-d6) is the deuterium-labeled 8-Chlorotheophylline (HY-W014203) . 8-Chlorotheophylline is an organic compound.
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Bensulfuron-methyl-d6 is a deuterated Bensulfuron-methyl (HY-B0870) (sulfonylurea pesticides). Bensulfuron-methyl-d6 can be used as an internal standard for the determination of pesticide residues by LC-MS[1].
Cipepofol-d6(Ciprofol-d6;HSK3486-d6) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
Norgestrel-d6 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives. Norgestrel-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mavacamten-d6(MYK461-d6;SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Olmesartan-d6(RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure[1][2].
N-Acetyl Norgestimate-d6 is the deuterium labeled N-Acetyl Norgestimate[1]. N-Acetyl Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
Cipepofol-d6-2(Ciprofol-d6-2;HSK3486-d6-2) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Ternidazole-d6 (hydrochloride) is the deuterium labeled Ternidazole hydrochloride. Ternidazole hydrochloride is a hydroxymetabolite of nitroimidazole, has antiprotozoic properties[1][2].
Eldecalcitol-d6 is the deuterium labeled Eldecalcitol. Eldecalcitol is an orally active analogue of active vitamin D used in the treatment of osteoporosis.
rel-Ritonavir-d6 (rel-ABT 538-d6;rel-RTV-d6) is the deuterium labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Norgestimate-d6 is the deuterium labeled Norgestimate. Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive[1][2]. Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Aminoadipic acid-d6 is deuterated labeled Aminoadipic acid (HY-113328). Aminoadipic acid is an intermediate in the metabolism of lysine and glycopurine.
Ciprofibrate-d6 is deuterium labeled Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha[1].
Podofilox-d6 is the deuterium labeled Podofilox. Podofilox (Podophyllotoxin) is a potent inhibitor of microtubule assembly and DNA topoisomerase II[1][2].
Fenofibric acid-d6 (FNF acid-d6) is the deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
Enasidenib-d6(AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
Ivabradine-d6 (hydrochloride) is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
Dydrogesterone-d6 is the deuterium labeled Dydrogesterone. Dydrogesterone is a potent, orally active progestogen indicated in a wide variety of gynaecological conditions related to progesterone deficiency.
Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
Tetracycline-d6 is the deuterium labeled Tetracycline. Tetracycline is a broad-spectrum antibiotic, exhibiting activity against a wide range of gram-positive and gram-negative bacteria.
Paraxanthine-d6 is the deuterium labeled Paraxanthine. Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.
Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
Picropodophyllin-d6(AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Elacestrant-d6(RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
Acamprosate-d6 (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems[1].
Bilastine-d6 is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria[1][2].
Irbesartan-d6 is the deuterium labeled Irbesartan. Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
Norethindrone-d6 is the deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea. Norethindrone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propionylpromazine-d6 (hydrochloride) is the deuterium labeled Propionylpromazine hydrochloride. Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease[1].
Rifaximin-d6 is the deuterium labeled Rifaximin. Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity[1][2].
Tetrahydrocortisone-d6 is the deuterium labeled Tetrahydrocortisone. Tetrahydrocortisone is a stress-induced hormone. Tetrahydrocortisone is also a urinary metabolite of Cortisone derived from the reduction of Cortisone by 5-reductase[1].
Piperaquine-d6 is the deuterium labeled Piperaquine[1]. Piperaquine is a bisquinoline antimalarial agent. Piperaquine can be used in antimalarial research in combination with Artemisinin[2][3].
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone[1]. 22-Hydroxy Mifepristone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Syringic acid-d6 is the deuterium labeled Syringic acid[1]. Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation[2][3].
Paricalcitol-d6 is the deuterium labeled Paricalcitol. Paricalcitol is a agent used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure[1].
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Maribavir-d6(1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[1][2].
(Rac)-Tenofovir-d6 is a labelled racemic Tenofovir. Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
L-Ornithine-d6 (hydrochloride) is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
Chlorotoluron-d6 is the deuterium labeled Chlorotoluron[1]. Chlorotoluron (Chlortoluron) is a substituted phenylurea herbicide, is widely used for selective weed control in cereals crops and is an environmental pollutant[2].
Piperaquine-d6 (tetraphosphate) is the deuterium labeled Piperaquine tetraphosphate. Piperaquine tetraphosphate is a bisquinoline antimalarial agent. Piperaquine phosphate can be used in antimalarial research in combination with Artemisinin[1][2].
Dobesilate-d6 (calcium) is deuterium labeled Calcium dobesilate. Calcium dobesilate, a vasoprotective, is widely used in chronic venous disease, diabetic retinopathy and the symptoms of haemorrhoidal attack in many countries.
Venlafaxine-d6 is the deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Flunisolide-d6 is the deuterium labeled Flunisolide. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
3,4-Dimethoxy-benzaldehyde-d6 is the deuterium labeled Veratraldehyde[1]. Veratraldehyde is an important chemical used in perfumery, agrochemical, and pharmaceutical industries.
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Choline-d6 (chloride) is the deuterium labeled Choline chloride. Choline chloride is an organic compound and a quaternary ammonium salt, an acyl group acceptor and choline acetyltransferase substrate, also is an important additive in feed especially for chickens where it accelerates growth.
Lanosterol-d6 is deuterium labeled Lanosterol. Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol s
Captan-d6 is the deuterium labeled Captan[1]. Captan is a common agricultural fungicide used to control Botrytis, Fusarium, Fusicoccum, Pythium. Captan enhances denitrifying and total culturable bacteria[2].
Rizatriptan-d6 (benzoate) is the deuterium labeled Rizatriptan benzoate. Rizatriptan benzoate is a 5-HT1 agonist triptan agent for the treatment of migraine headaches[1][2].
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
25-Hydroxycholesterol-d6(25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells[1][2].
Desmosterol-d6 is the deuterium labeled Desmosterol. Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism[1].
Pirimicarb-d6 is the deuterium labeled Diuron. Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male
Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
L-Citrulline-d6 is the deuterium labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea[1][2].
Baquiloprim-d6 is deuterium labeled Baquiloprim. Baquiloprim, an antibiotic, is a selective inhibitor of bacterial dihydrofolate reductases. Baquiloprim possesses in vitro bacteriostatic activity against both Gram-negative and Gram-positive bacteria[1][2].
Dapoxetine-d6 is the deuterium labeled Dapoxetine[1]. Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE)[2].
2-Methylpyrazine-d6 is the deuterium labeled 2-Methylpyrazine[1]. 2-Methylpyrazine is a kind of alkylpyrazine that can be identified in roasted red pepper seed oils[2].
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Verapamil-d6(CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
1,3-Propanediol-d6 is the deuterium labeled 1,3-Propanediol[1]. 1,3-Propanediol is produced in nature by the fermentation of glycerol in microorganism[2].
Methylprednisolone acetate-d6 is the deuterium labeled Methylprednisolone acetate (HY-13681). Methylprednisolone acetate, a prednisolone derivative, is a corticosteroid hormone. Methylprednisolone acetate can relieve pain and swelling that occurs with arthritis and other joint disorders in vivo .
l-α-tocopherol acetate- 13C4,d6 is the 13C- and deuterium-labeled l-α-tocopherol acetate. l-α-tocopherol acetate is a natural tocopherol and has potent antioxidant activities[1].
Dansyl-2-(2-azidoethoxy)ethanamine-d6 is the deuterium labeled Dansyl-2-(2-azidoethoxy)ethanamine[1]. Dansyl-2-(2-azidoethoxy)ethanamine-d6 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Esomeprazole-d6 sodium is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte[1].
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
Hexazinone-d6 is the deuterium labeled Hexazinone[1]. Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis[2].
Leucocrystal violet-d6 is the deuterium labeled Leucocrystal violet[1]. Leucocrystal violet is a triphenylmethane dye which can be used to detect antimony in environmental and biological samples using spectrophotometric techniques[2][3].
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
Isoxsuprine-d6 (hydrochloride) is the deuterium labeled Isoxsuprine hydrochloride. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
Diltiazem-d6 is the deuterium labeled Diltiazem. Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
α-Tocopherol-d6 (acetate) is the deuterium labeled D-α-Tocopherol acetate. D-α-Tocopherol acetate (D-Vitamin E acetate) can be hydrolyzed to d-alpha-tocopherol (VE) and absorbed in the small intestine[1].
Dehydroepiandrosterone sulfate-d6 (sodium dihydrate) is the deuterium labeled tert-Butyl N-[(1S)-1-[Methoxy(methyl)carbamoyl]-2-phenylethyl]carbamate[1].
Glutaric acid-d6 is the deuterium labeled Glutaric acid. Glutaric acid is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
4-Methylcatechol-d6 is the deuterium labeled 4-Methylcatechol[1]. 4-Methylcatechol, a metabolite of p-toluate, is a substrate as well as a suicide inhibitor of Catechol 2,3-Dioxygenase[2].
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Dimethyl fumarate-d6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression[1][2][3][4][5][6].
Risdiplam-hydroxylate-d6 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels .
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Metolachlor-d6 is the deuterium labeled Metolachlor[1]. Metolachlor is a pre-emergent selective, chloroacetanilide herbicide for the control of a variety of annual grass and broad leaf weeds in corn and other crops. Metolachlor is a chiral herbicide consisting of four stereoisomers[2][3].
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
H-Abu-OH-d6 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
Melitracen-d6 (hydrochloride) is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space[1][2].
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].
Nicosulfuron-d6 is the deuterium labeled Nicosulfuron[1]. Nicosulfuron is a selective herbicide belonging to the sulfonylurea family. Nicosulfuron is commonly used as a post-emergence herbicide to protect maize crops from weeds. Nicosulfuron inhibits acetolactate synthase (ALS) enzyme activity[2].
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins[1].
Alendronic acid-d6 is the deuterium labeled Alendronic acid. Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease[1].
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
D-Ribose-d6 is the deuterium labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein gl
Methyl syringate-d6 is the deuterium labeled Methyl syringate[1]. Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist[2][3][4].
2-Methylsuccinic acid-d6 is the deuterium labeled 2-Methylsuccinic acid[1]. 2-Methylsuccinic acid is a normal metabolite in human fluids and the main biochemical measurable features in ethylmalonic encephalopathy[2][3].
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Metoprolol-d6 (tartrate) is the deuterium labeled Metoprolol tartrate. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3][4].
4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds[1][2].
Chlorprothixene-d6 (hydrochloride) is the deuterium labeled Chlorprothixene hydrochloride. Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
Metalaxyl-d6 is the deuterium labeled Metalaxyl. Metalaxyl is a fungicide that inhibits protein synthesis in fungi. Metalaxyl inhibits the growth of potato blight (P. infestans) fungal isolates from Serbian potato fields (EC50s=0.3-3.9 μg/mL).
Trandolaprilate-d6 is the deuterium labeled Trandolaprilate[1]. Trandolaprilate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity[2][3].
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
3-Mercapto-3-methylbutan-1-ol-d6 is the deuterium labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Dimethoate-d6 is the deuterium labeled Dimethoate. Dimethoate is an effective systemic insecticide for use on plants, has shown promise as a chemotherapeutic agent for control of cattle grubs and certain other insect pests of farm animals, and has high contact toxicity to house-flies and many other insects[1].
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification[1][2].
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit[1]. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis[2].
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
DL-Norepinephrine-d6 (hydrochloride) is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension[1].
4-Epitetracycline-d6 is deuterated labeled 4-Epitetracycline hydrochloride (HY-136443) 4-Epitetracycline hydrochloride is an epimer of Tetracycline (HY-A0107). Tetracycline can undergo epimerization insolution to 4-Epitetracycline hydrochloride, which shows a much lower antibiotic activity.
Calcifediol-d6 (monohydrate) is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), a major circulating metabolite of vitamin D3, is a potent VDR ligand .
1,3-Dimethoxybenzene-d6 is the deuterium labeled 1,3-Dimethoxybenzene[1]. 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds[2].
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone[1]. 1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity[2].
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Propane-1,2,3-triyl tripalmitate-d6 is the deuterium labeled Propane-1,2,3-triyl tripalmitate. Propane-1,2,3-triyl tripalmitate is an endogenous metabolite.
(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
DL-dithiothreitol-d6 is the deuterium labeled DL-dithiothreitol[1]. DL-dithiothreitol (DTT) is a reducing agent. DL-dithiothreitol forms a stable six-membered ring with an internal disulfide bond once oxidized[2].
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
Ranitidine-d6 (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].
Enterolactone-d6 is the deuterium labeled Enterolactone. Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity[1]. Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis[2].
Erythromycin-d6 is the deuterium labeled Erythromycin. Erythromycin is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Fenitrothion-d6 is the deuterium labeled Fenitrothion[1]. Fenitrothion, one of the most widely used organophosphorus pesticides, is a cholinesterase inhibiting insecticide/acaricid. Fenitrothion is widely used, as a broad-spectrum insecticide, on cotton crops, vegetables crops, fruit crops, and field crops especially paddy. Fenitrothion leads to accumulation of nitrophenols[2][3].
Pirimiphos-methyl-d6 is the deuterium labeled Pirimiphos-methyl. Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains[1][2][3].
Metalaxyl-M-d6 is the deuterium labeled Metalaxyl-M[1]. Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division[2].
(Rac)-Zearalenone-d6 is the deuterium labled Zearalenone (HY-103447). Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D[1][2].
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
Diacerein-d6 is the deuterium labeled Diacerein[1]. Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases[2].
Bezafibrate-d6 is the deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Dihomo-γ-linolenic acid-d6(DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
1-(4-Hydroxyphenyl)-2-((4-(4-hydroxyphenyl)butan-2-yl)amino)ethanone-d6 (hydrochloride) is the deuterium labeled 1-(4-Hydroxyphenyl)-2-((4-(4-hydroxyphenyl)butan-2-yl)amino)ethanone hydrochloride[1].
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities[1][2].
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
5-Hydroxyindole-3-acetic acid-d6 is the deuterium labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].
Toremifene-d6 (citrate) is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Canagliflozin-d6 is the deuterium labeled Canagliflozin[1]. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[2].
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity[1][2].
Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].
Buprofezin-d6 is the deuterium labeled Buprofezin. Buprofezin is a broad-spectrum insecticide and chitin synthesis inhibitor that targets developmental stage coleopteran pests.Buprofezin promotes the conversion of energy metabolism from the aerobic tricarboxylic acid (TCA) cycle and oxidative phosphorylation to anaerobic glycolysis. Buprofezin also promotes the production of reactive oxygen species (ROS) by inhibiting cytochrome c oxidase[1][2].
Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
Tricin-d6 is the deuterium labeled Tricin[1]. Tricin is a natural flavonoid present in large amounts in Triticum aestivum. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7[2][3][4].
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Ribociclib-d6 is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Ribociclib-d6 (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Umifenovir-d6 (hydrochloride) is the deuterium labeled Umifenovir hydrochloride. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity[3].
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Bisphenol A-d6 is the deuterium labeled Bisphenol A. Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders[1][2][3].
Squalene-d6 is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis[1][2][3][4][5].
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
Melengestrol acetate-d6 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate[1]. DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition[2][3].
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
(7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is the deuterium labeled MCA[1]. MCA is a coumarin derivative. MCA quantitates platelet-activating factor by high-performance liquid chromatography with fluorescent detection. MCA can modify FRET peptide substrates for analyzing protease activities[2][3]. (7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system[1].
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87[1][2].
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance[1][2].
Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
Irbesartan-d6-1 is the deuterium labeled Irbesartan[1]. Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease[2].
Sucralose-d6 is deuterium labeled Sucralose. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents[1][2].
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride[1]. Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2][3][4][5][6][7].
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
N-Hydroxy (E)-2-(4-methoxybenzoxy)-4-methoxy-3-prenylcinnamamide-d6 is the deuterium labeled N-Hydroxy (E)-2-(4-methoxybenzoxy)-4-methoxy-3-prenylcinnamamide[1].
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
(rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1][2].
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
N1-Acetylspermidine-d6 (hydrochloride) is the deuterium labeled N1-Acetylspermidine hydrochloride. N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA[1][2][3].
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine[1]. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[2].
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome[1][2].
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
Dalbavancin-d6 is the deuterium labeled Dalbavancin[1]. Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[2][3].
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects[1][2][3].
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol[1]. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents[2].
Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
5α-Cholesta-7,24-dien-3β-ol-d6 is deuterium labeled 5α-Cholesta-7,24-dien-3β-ol. 5α-Cholesta-7,24-dien-3β-ol, a sterol, can be found in hamster cauda epididymal mature spermatozoa[1].
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels[1].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment .
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
(rac)-Dobutamine-d6 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
(Rac)-Bedaquiline-d6is the deuterium labeledBedaquiline(HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
3-epi-25-Hydroxy Vitamin D3-d6is the deuterium labeled3-epi-25-Hydroxy Vitamin D3(HY-142140) . 3-epi-25-Hydroxy Vitamin D3 is the vitamin D metabolite, while vitamin D metabolism highly dependent on macrophage polarization. The C3-epimerase pathway for vitamin D is active in macrophages .
Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
Maxacalcitol-d66 is the deuterated form of Maxacalcitol (22-Oxacalcitriol), which is a non-calcemic vitamin D3 analog and VDR ligand of VDR-like receptors.
4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Norgestrel-d6 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives. Norgestrel-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
N-Acetyl Norgestimate-d6 is the deuterium labeled N-Acetyl Norgestimate[1]. N-Acetyl Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norgestimate-d6 is the deuterium labeled Norgestimate. Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive[1][2]. Norgestimate-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norethindrone-d6 is the deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea. Norethindrone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Dansyl-2-(2-azidoethoxy)ethanamine-d6 is the deuterium labeled Dansyl-2-(2-azidoethoxy)ethanamine[1]. Dansyl-2-(2-azidoethoxy)ethanamine-d6 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is the deuterium labeled MCA[1]. MCA is a coumarin derivative. MCA quantitates platelet-activating factor by high-performance liquid chromatography with fluorescent detection. MCA can modify FRET peptide substrates for analyzing protease activities[2][3]. (7-Methoxy-2-oxo-2H-chromen-4-yl)-acetic acid-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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