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competitive manner

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73

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4

Peptides

10

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7

Isotope-Labeled Compounds

1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101631
    Levophacetoperane hydrochloride

    		Dopamine Transporter Neurological Disease
    Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
    Levophacetoperane hydrochloride
  • HY-N3320
    Marmin

    		Others Neurological Disease
    Marmin is a coumarin, that can be isolated from the immature bark of Aegle marmelos Correa. Marmin antagonizes the Histamine (HY-B1204)-induced contraction in competitive manner .
    Marmin
  • HY-W007686
    Imidazoleacetic acid hydrochloride
    2 Publications Verification

    Imidazolyl-4-acetic acid hydrochloride

    		 Endogenous Metabolite GABA Receptor Neurological Disease
    Imidazoleacetic acid hydrochloride is a γ-aminobutyric acid receptor agonist. Imidazoleacetic acid hydrochloride inhibits GABA-T in a non-competitive manner, with a Ki value of 0.34 mM. Imidazoleacetic acid hydrochloride increases total free GABA in brain .
    Imidazoleacetic acid hydrochloride
  • HY-119409
    Levophacetoperane

    Phacetoperane free base

    		 Dopamine Transporter Neurological Disease
    Levophacetoperane (Phacetoperane free base) competitively inhibits the uptake of norepinephrin and dopamine .
    Levophacetoperane
  • HY-N2087
    Ligupurpuroside A

    		Lipase Metabolic Disease
    Ligupurpuroside A is an active product that can be extracted from Ligustrum robustum. Ligupurpuroside A acts as a natural inhibitor of lipase in a competitive manner .
    Ligupurpuroside A
  • HY-115939
    Urease-IN-2

    		Bacterial Urease Infection
    Urease-IN-2 (compound 8g) is a non-competitive urease inhibitor with an IC50 of 0.94 μM and a Ki of 1.6 μM. Urease-IN-2 inhibits the Jack bean urease (JBU) in a non-competitive manner .
    Urease-IN-2
  • HY-124777
    NPD4456

    		HIV Infection
    NPD4456 (Compound 3) is a 3-phenylcoumarin Vpr inhibitor. NPD4456 binds to Vpr in a competitive manner. NPD4456 inhibits HIV-1 viral infection .
    NPD4456
  • HY-N2383
    Validamine

    (1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol

    		 Glycosidase Metabolic Disease
    Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
    Validamine
  • HY-W424730
    HA-966 hydrochloride

    		iGluR Others
    HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
    HA-966 hydrochloride
  • HY-149775
    Urease-IN-10

    		Bacterial Urease Infection
    Urease-IN-10 (Conjugate 4) is a competitive Urease inhibitor, with an IC50 of 3.59±0.07 μM and a Ki of 7.45 μM. Urease-IN-10 is a conjugate consisting of Diclofenac (HY-15036) and Sulfanilamide (HY-B0242). Diclofenac-sulfanilamide inhibits the Jack bean urease(JBU) in a competitive manner .
    Urease-IN-10
  • HY-P3853
    GR 87389

    		Neurokinin Receptor Neurological Disease
    GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
    GR 87389
  • HY-101169
    Tetrindole mesylate

    		Monoamine Oxidase Neurological Disease
    Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
    Tetrindole mesylate
  • HY-P1178
    Cyclotraxin B
    3 Publications Verification

    		 Trk Receptor p38 MAPK Neurological Disease
    Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
    Cyclotraxin B
  • HY-157124
    Tyrosinase-IN-19

    		Tyrosinase Metabolic Disease
    Tyrosinase-IN-19 (compound 9) is a competitive tyrosinase inhibitor. Tyrosinase-IN-19 has strong antioxidant activities against ROS, ABTS+, and DPPH radicals. Tyrosinase-IN-19 suppresses tyrosinase expression in a dose-dependent manner .
    Tyrosinase-IN-19
  • HY-N9506
    Anisatin

    		GABA Receptor Neurological Disease
    Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM .
    Anisatin
  • HY-P1178A
    Cyclotraxin B TFA

    		Trk Receptor Neurological Disease
    Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects .
    Cyclotraxin B TFA
  • HY-109097
    Otaplimastat

    SP-8203

    		 MMP iGluR Neurological Disease
    Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury .
    Otaplimastat
  • HY-118131
    PKR-IN-C51

    		Ser/Thr Protease Infection
    PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages .
    PKR-IN-C51
  • HY-169422
    GSK4418959

    IDE275

    		 DNA/RNA Synthesis Cancer
    GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer .
    GSK4418959
  • HY-101544
    ARQ 069

    		FGFR Cancer
    ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .
    ARQ 069
  • HY-W007686R
    Imidazoleacetic acid hydrochloride (Standard)

    Imidazolyl-4-acetic acid hydrochloride (Standard)

    		 Reference Standards Endogenous Metabolite GABA Receptor Metabolic Disease
    Imidazoleacetic acid (hydrochloride) (Standard) is the analytical standard of Imidazoleacetic acid (hydrochloride). This product is intended for research and analytical applications. Imidazoleacetic acid hydrochloride is a γ-aminobutyric acid receptor agonist. Imidazoleacetic acid hydrochloride inhibits GABA-T in a non-competitive manner, with a Ki value of 0.34 mM. Imidazoleacetic acid hydrochloride increases total free GABA in brain[1][2][3].
    Imidazoleacetic acid hydrochloride (Standard)
  • HY-13816
    NU6027

    		CDK ATM/ATR Cancer
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner .
    NU6027
  • HY-10119
    Vorapaxar
    10+ Cited Publications

    SCH 530348

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar
  • HY-106840A
    L-365260 hemihydrate
    1 Publications Verification

    		 Cholecystokinin Receptor Neurological Disease Metabolic Disease
    L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
    L-365260 hemihydrate
  • HY-10119A
    Vorapaxar sulfate
    10+ Cited Publications

    SCH 530348 sulfate

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar sulfate
  • HY-W011834
    2'-O-Methylcytidine

    		HCV DNA/RNA Synthesis Infection
    2'-O-Methylcytidine is an orally active 2'-substituted nucleoside as a inhibitor of HCV replication with antiviral activity. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
    2'-O-Methylcytidine
  • HY-B0607
    Nitisinone
    2 Publications Verification

    NTBC; Nitisone; SC0735

    		 HPPD Metabolic Disease
    Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
    Nitisinone
  • HY-115750
    Nω-allyl-L-arginine

    		NO Synthase Neurological Disease
    Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
    Nω-allyl-L-arginine
  • HY-146333
    TRAP-6-IN-1

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner .
    TRAP-6-IN-1
  • HY-107001
    DPC 961

    (S)-DPC 961; DMP 961

    		 HIV Reverse Transcriptase Infection
    DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS .
    DPC 961
  • HY-N10403
    4-Hydroxyestradiol
    1 Publications Verification

    4-Hydroxy-17β-estradiol

    		 Drug Metabolite Endogenous Metabolite Cancer
    4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
    4-Hydroxyestradiol
  • HY-N4042
    Hirsutenone

    		PI3K ERK Inflammation/Immunology Cancer
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity .
    Hirsutenone
  • HY-114641A
    BIIL-260 hydrochloride
    1 Publications Verification

    		 Leukotriene Receptor Inflammation/Immunology
    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM .
    BIIL-260 hydrochloride
  • HY-114641
    BIIL-260

    		Leukotriene Receptor Inflammation/Immunology
    BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with the Ki value of 1.7 nM .
    BIIL-260
  • HY-P3678
    Neuropeptide Y (18-36) (porcine)

    		Neuropeptide Y Receptor Cardiovascular Disease Neurological Disease
    Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
    Neuropeptide Y (18-36) (porcine)
  • HY-10572A
    (R)-Efavirenz

    (R)-DMP 266; (R)-EFV; (R)-L-743726

    		 Reverse Transcriptase Infection
    (R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
    (R)-Efavirenz
  • HY-13011
    Alectinib
    Maximum Cited Publications
    36 Publications Verification

    CH5424802; RO5424802; RG7853

    		 Anaplastic lymphoma kinase (ALK) Cancer
    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 . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib
  • HY-15959
    Savolitinib
    5+ Cited Publications

    Volitinib; HMPL-504; AZD-6094

    		 c-Met/HGFR Cancer
    Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
    Savolitinib
  • HY-10119S
    Vorapaxar-d5

    SCH 530348-d5

    		 Protease Activated Receptor (PAR) Isotope-Labeled Compounds Cardiovascular Disease
    Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar-d5
  • HY-B0091A
    Adapalene sodium salt

    CD 271 sodium salt

    		 RAR/RXR Autophagy Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
    Adapalene sodium salt
  • HY-B0091
    Adapalene
    4 Publications Verification

    CD271

    		 RAR/RXR Autophagy Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
    Adapalene
  • HY-10119R
    Vorapaxar (Standard)

    SCH 530348 (Standard)

    		 Reference Standards Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar (Standard)
  • HY-106840
    L-365260
    1 Publications Verification

    		 Cholecystokinin Receptor Neurological Disease Metabolic Disease
    L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
    L-365260
  • HY-13011A
    Alectinib Hydrochloride
    Maximum Cited Publications
    36 Publications Verification

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 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 . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib Hydrochloride
  • HY-10119AR
    Vorapaxar sulfate (Standard)

    SCH 530348 sulfate (Standard)

    		 Reference Standards Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar sulfate (Standard)
  • HY-B0607R
    Nitisinone (Standard)

    NTBC (Standard); Nitisone (Standard); SC0735 (Standard)

    		 HPPD Reference Standards Metabolic Disease
    Nitisinone (Standard) is the analytical standard of Nitisinone. This product is intended for research and analytical applications. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
    Nitisinone (Standard)
  • HY-13011S1
    Alectinib-d6

    CH5424802-d6; RO5424802-d6; AF802-d6

    		 Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK) Cancer
    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 . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib-d6
  • HY-100201
    A-196
    5+ Cited Publications

    		 Histone Methyltransferase Cancer
    A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
    A-196
  • HY-W017158R
    Melilotic acid (Standard)

    		Reference Standards Endogenous Metabolite Metabolic Disease
    Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Melilotic acid (Standard)
  • HY-W011834S
    2'-O-Methylcytidine-d3

    		Isotope-Labeled Compounds HCV Infection
    2'-O-Methylcytidine-d3 is deuterium labeled 2'-O-Methylcytidine (HY-W011834). 2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
    2'-O-Methylcytidine-d3

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