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Aminopeptidase N Ligand (CD13) NGR peptide is a polypeptide targeting CD13 and can be used as a carrier to mediate intracellular transmission. Aminopeptidase N Ligand (CD13) NGR peptide is often used in cancer research .
BC-05 is an orally active and potent inhibitor of CD13 and proteasome. BC-05 has an IC50 value of 0.13 μM for human CD13 and an IC50 value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research .
A Aminopeptidase N (rat) (APN/CD13) is a Zn 2+ dependent membrane-bound ectopeptidase that degrades preferentially proteins and peptides with a N-terminal neutral amino acid .
Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
NGR peptide Trifluoroacetatecontaining the Asn-Gly-Arg (NGR) motif. NGR peptide Trifluoroacetate binds to APN/CD13. NGR peptide Trifluoroacetate is directly conjugated to imaging agents that can be used for tumor imaging .
NGR peptide containing the Asn-Gly-Arg (NGR) motif. NGR peptide binds to APN/CD13. NGR peptide is directly conjugated to imaging agents that can be used for tumor imaging .
Azelastine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Azelastine hydrochloride. Azelastine- 13C,d3 (hydrochloride), an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine- 13C,d3 (hydrochloride) can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Cytidine-5'-triphosphate- 13C,d1 (Cytidine triphosphate- 13C,d1 dilithium; 5'-CTP- 13C,d1) dilithium is deuterium and 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid[1]. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats[2].
L-Methionine- 13C,d5 is the 13C- and deuterium labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
L-Methionine- 13C,d3 is the 13C- and deuterium labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
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.
2-Methoxyestrone- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestrone. 2-Methoxyestrone is a methoxylated catechol estrogen and metabolite of estrone, with a pKa of 10.81.
Yohimbine- 13C,d3 is the 13C- and deuterium labeled Yohimbine. Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.
BIBF 1202- 13C,d3 is the 13C- and deuterium labeled BIBF 1202. BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
Alizapride- 13C,d3 (hydrochloride) is deuterium labeled Alizapride (hydrochloride). Alizapride hydrochloride is a dopamine receptor antagonist with prokinetic and antiemetic effects which can also be used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
(Rac)-Vazegepant- 13C,d3 is the C13 and deuterium labeled (Rac)-Vazegepant. Vazegepant (HY-134992) is the first intranasal CGRP receptor antagonist for the study the acute research of migraine .
D-Mannose- 13C,d-2 is the deuterium and 13C labeled D-Mannose. D-Mannose is a carbohydrate, which plays an important role in human metabolism, especially in the glycosylationof specific prote[1][2].
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
Famotidine- 13C,d3 is the 13C- and deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Sofosbuvir- 13C,d3 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.
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
Doxorubicin- 13C,d3 (TFA) is the deuterium and 13C labeled Doxorubicin. Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stoppin
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Ametryn- 13C,d3 is the 13C- and deuterium labeled Ametryn. Ametryn, a member of the Triazine chemical family, is a herbicide which inhibits photosynthesis and other enzymatic processes. Ametryn is effective against annual broadleaf weeds and grasses[1].
Ac-rC Phosphoramidite- 13C,d1 is deuterium and 13C-labeled Ac-rC Phosphoramidite (HY-W042357). Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA).
Ritonavir- 13C,d3 is the 13C- and 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.
Zafirlukast- 13C,d3 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.
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.
Meloxicam- 13C,d3 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
Lercanidipine- 13C,d3-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[1][2][3].
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
Azelastine- 13C,d3 is deuterium labeled Azelastine. Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
(R)-Clevidipine- 13C,d3 is the deuterium and 13C labeled Clevidipine[1]. Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension[2].
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and 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].
(Rac)-Hesperetin- 13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
(±)-Naproxen- 13C,d3 is the deuterium and 13C labeled (±)-Naproxen[1]. (±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.
Lercanidipine- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Lercanidipine hydrochloride[1]. Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[2][3][4].
Avobenzone- 13C,d3 is the 13C- and deuterium labeled Avobenzone. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist[1][2].
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Sodium 3-methyl-2-oxobutanoate- 13C,d4 is the deuterium and 13C labeled Sodium 3-methyl-2-oxobutanoate[1]. Sodium 3-methyl-2-oxobutanoate is a precursor of pantothenic acid in Escherichia coli[2][3][4].
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
1-Methylxanthine- 13C,d3 is the 13C- and deuterium labeled 1-Methylxanthine. 1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP)[1]. 1-Methylxanthine enhances the radiosensitivity of tumor cells[2].
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death[1][2].
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
Methyl Eugenol- 13C,d3 is the 13C- and deuterium labeled Methyl Eugenol. Methyl Eugenol, a phenylpropanoid chemical in leaves, fruits, stems, and/or roots, may be released when that corresponding part of a plant is damaged as a result of feeding by an herbivore. Methyl Eugenol is used for male annihilation of the oriental fruit fly[1].
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) 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, respectively.
Sodium 3-methyl-2-oxobutanoate- 13C,d4-1 is the deuterium and 13C labeled Sodium 3-methyl-2-oxobutanoate[1]. Sodium 3-methyl-2-oxobutanoate is a precursor of pantothenic acid in Escherichia coli[2][3][4].
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
Erythromycin- 13C,d3 is the 13C- and 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].
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Methocarbamol- 13C,d3 is the 13C- and deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib[1]. 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[2][3].
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Carprofen- 13C,d3 is the deuterium and 13C labeled Carprofen[1]. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[2][3][4].
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Asenapine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain[1][2][3].
Regorafénib N-oxyde (M2)- 13C,d3 is the 13C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
Pelubiprofen- 13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].
Carbamazepine 10,11-epoxide- 13C,d2 is the deuterium labeled Carbamazepine 10,11-epoxide-C13. Carbamazepine 10,11-epoxide-C13 is a 13C-labled Carbamazepine 10,11-epoxide. Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures[1][2].
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency. Zidovudine-13C,d3 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.
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2][3].
NGR peptide Trifluoroacetatecontaining the Asn-Gly-Arg (NGR) motif. NGR peptide Trifluoroacetate binds to APN/CD13. NGR peptide Trifluoroacetate is directly conjugated to imaging agents that can be used for tumor imaging .
Aminopeptidase N Ligand (CD13) NGR peptide is a polypeptide targeting CD13 and can be used as a carrier to mediate intracellular transmission. Aminopeptidase N Ligand (CD13) NGR peptide is often used in cancer research .
NGR peptide containing the Asn-Gly-Arg (NGR) motif. NGR peptide binds to APN/CD13. NGR peptide is directly conjugated to imaging agents that can be used for tumor imaging .
Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
Aminopeptidase N/APN proteins act as aminopeptidases with broad specificity, assisting in the final stages of peptide digestion and processing of various peptides, including the hormones angiotensin III/IV and neuropeptides. Aminopeptidase N/APN Protein, Mouse (HEK293, His) is the recombinant mouse-derived Aminopeptidase N/APN protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Aminopeptidase N/APN Protein, Mouse (HEK293, His) is 898 a.a., with molecular weight of 110-130 kDa.
Aminopeptidase N/APN Protein, Human (HEK 293, His) is a recombinant aminopeptidase N/APN protein with a His tag. APN (also known as CD13) is a Zn2+ dependent membrane-bound ectopeptidase that degrades preferentially proteins and peptides with a N-terminal neutral amino acid.
Aminopeptidase N/APN protein is a disulfide-bonded homotrimer functioning as a broad specificity aminopeptidase. It plays a crucial role in peptide digestion, peptide processing, antigen presentation, angiogenesis, and cholesterol crystallization. APN protein also interacts with the amino acid transporter SLC6A19 and acts as a receptor for human coronavirus 229E/HCoV-229E during infection. Aminopeptidase N/APN Protein, Human (HEK293, His) is the recombinant human-derived Aminopeptidase N/APN protein, expressed by HEK293, with C-His labeled tag. The total length of Aminopeptidase N/APN Protein, Human (HEK293, His) is 899 a.a., with molecular weight of 130-140 kDa.
Aminopeptidase N/APN protein is a disulfide-bonded homotrimer functioning as a broad specificity aminopeptidase. It plays a crucial role in peptide digestion, peptide processing, antigen presentation, angiogenesis, and cholesterol crystallization. APN protein also interacts with the amino acid transporter SLC6A19 and acts as a receptor for human coronavirus 229E/HCoV-229E during infection. Aminopeptidase N/APN Protein, Human (I603M, HEK293, His) is the recombinant human-derived Aminopeptidase N/APN protein, expressed by HEK293 , with C-His labeled tag and I603M mutation. The total length of Aminopeptidase N/APN Protein, Human (I603M, HEK293, His) is 899 a.a., with molecular weight of 135-140 kDa.
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
Azelastine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Azelastine hydrochloride. Azelastine- 13C,d3 (hydrochloride), an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine- 13C,d3 (hydrochloride) can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Cytidine-5'-triphosphate- 13C,d1 (Cytidine triphosphate- 13C,d1 dilithium; 5'-CTP- 13C,d1) dilithium is deuterium and 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid[1]. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats[2].
L-Methionine- 13C,d5 is the 13C- and deuterium labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
L-Methionine- 13C,d3 is the 13C- and deuterium labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
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.
2-Methoxyestrone- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestrone. 2-Methoxyestrone is a methoxylated catechol estrogen and metabolite of estrone, with a pKa of 10.81.
Yohimbine- 13C,d3 is the 13C- and deuterium labeled Yohimbine. Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.
BIBF 1202- 13C,d3 is the 13C- and deuterium labeled BIBF 1202. BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
Alizapride- 13C,d3 (hydrochloride) is deuterium labeled Alizapride (hydrochloride). Alizapride hydrochloride is a dopamine receptor antagonist with prokinetic and antiemetic effects which can also be used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
(Rac)-Vazegepant- 13C,d3 is the C13 and deuterium labeled (Rac)-Vazegepant. Vazegepant (HY-134992) is the first intranasal CGRP receptor antagonist for the study the acute research of migraine .
D-Mannose- 13C,d-2 is the deuterium and 13C labeled D-Mannose. D-Mannose is a carbohydrate, which plays an important role in human metabolism, especially in the glycosylationof specific prote[1][2].
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
Famotidine- 13C,d3 is the 13C- and deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Sofosbuvir- 13C,d3 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.
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
Doxorubicin- 13C,d3 (TFA) is the deuterium and 13C labeled Doxorubicin. Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stoppin
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Ametryn- 13C,d3 is the 13C- and deuterium labeled Ametryn. Ametryn, a member of the Triazine chemical family, is a herbicide which inhibits photosynthesis and other enzymatic processes. Ametryn is effective against annual broadleaf weeds and grasses[1].
Ac-rC Phosphoramidite- 13C,d1 is deuterium and 13C-labeled Ac-rC Phosphoramidite (HY-W042357). Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA).
Ritonavir- 13C,d3 is the 13C- and 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.
Zafirlukast- 13C,d3 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.
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.
Meloxicam- 13C,d3 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
Lercanidipine- 13C,d3-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[1][2][3].
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
Azelastine- 13C,d3 is deuterium labeled Azelastine. Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
(R)-Clevidipine- 13C,d3 is the deuterium and 13C labeled Clevidipine[1]. Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension[2].
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and 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].
(Rac)-Hesperetin- 13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
(±)-Naproxen- 13C,d3 is the deuterium and 13C labeled (±)-Naproxen[1]. (±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.
Lercanidipine- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Lercanidipine hydrochloride[1]. Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[2][3][4].
Avobenzone- 13C,d3 is the 13C- and deuterium labeled Avobenzone. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist[1][2].
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Sodium 3-methyl-2-oxobutanoate- 13C,d4 is the deuterium and 13C labeled Sodium 3-methyl-2-oxobutanoate[1]. Sodium 3-methyl-2-oxobutanoate is a precursor of pantothenic acid in Escherichia coli[2][3][4].
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
1-Methylxanthine- 13C,d3 is the 13C- and deuterium labeled 1-Methylxanthine. 1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP)[1]. 1-Methylxanthine enhances the radiosensitivity of tumor cells[2].
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death[1][2].
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
Methyl Eugenol- 13C,d3 is the 13C- and deuterium labeled Methyl Eugenol. Methyl Eugenol, a phenylpropanoid chemical in leaves, fruits, stems, and/or roots, may be released when that corresponding part of a plant is damaged as a result of feeding by an herbivore. Methyl Eugenol is used for male annihilation of the oriental fruit fly[1].
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) 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, respectively.
Sodium 3-methyl-2-oxobutanoate- 13C,d4-1 is the deuterium and 13C labeled Sodium 3-methyl-2-oxobutanoate[1]. Sodium 3-methyl-2-oxobutanoate is a precursor of pantothenic acid in Escherichia coli[2][3][4].
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
Erythromycin- 13C,d3 is the 13C- and 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].
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Methocarbamol- 13C,d3 is the 13C- and deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib[1]. 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[2][3].
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Carprofen- 13C,d3 is the deuterium and 13C labeled Carprofen[1]. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[2][3][4].
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Asenapine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain[1][2][3].
Regorafénib N-oxyde (M2)- 13C,d3 is the 13C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
Pelubiprofen- 13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].
Carbamazepine 10,11-epoxide- 13C,d2 is the deuterium labeled Carbamazepine 10,11-epoxide-C13. Carbamazepine 10,11-epoxide-C13 is a 13C-labled Carbamazepine 10,11-epoxide. Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures[1][2].
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency. Zidovudine-13C,d3 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.
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2][3].
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency. Zidovudine-13C,d3 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.
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