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CYP3A activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Autophagy (4) Bacterial (1) Cytochrome P450 (18) DNA/RNA Synthesis (1) Drug Metabolite (2) Endogenous Metabolite (2) ERK (2) Estrogen Receptor/ERR (1) GABA Receptor (8) Histamine Receptor (6) Isotope-Labeled Compounds (7) Reactive Oxygen Species (ROS) (2) Reference Standards (9) ROCK (1) STAT (2) Thrombopoietin Receptor (7) Virus Protease (2)
By Research Areas:	Cancer (15) Cardiovascular Disease (4) Infection (3) Inflammation/Immunology (8) Metabolic Disease (9) Neurological Disease (14)
Click Chemistry:	Tetrazine (1)

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-N0693

Schisandrin A 10+ Cited Publications Schizandrin-A; Wuweizisu-A; Deoxyschizandrin	Cytochrome P450 Autophagy Virus Protease	Inflammation/Immunology Cancer
Schisandrin A inhibits *CYP3A* activity with an IC₅₀ of 6.60 μM and K_i of 5.83 μM, respectively.

HY-B0696A

Tiagabine hydrochloride NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride	GABA Receptor	Neurological Disease
Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-N0692

Schisandrol B 2 Publications Verification Gomisin-A; TJN-101; Wuweizi alcohol-B	Reactive Oxygen Species (ROS) Cytochrome P450 Autophagy	Cancer
Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and *CYP3A* and also has anti-inflammatory, anti-diabetic and antioxidant activities .

HY-B0696

Tiagabine NO050328; NO328; TGB	GABA Receptor	Neurological Disease
Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-13463

Avatrombopag 5 Publications Verification AKR-501; E5501; YM477	Thrombopoietin Receptor	Inflammation/Immunology Cancer
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-A0069

Doxylamine succinate	Histamine Receptor Cytochrome P450	Neurological Disease Metabolic Disease
Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of *CYP2B, CYP2A, CYP3A* and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .

HY-113327

1,3,7-Trimethyluric acid	Endogenous Metabolite	Cancer
1,3,7-Trimethyluric acid is the metabolite of caffeine. The metabolic ratio 1,3,7-Trimethyluric acid to caffeine can be evaluated as a biomarker to describe variability in CYP3A activity in a cohort .

HY-W019847

Azamulin	Cytochrome P450	Infection Metabolic Disease
Azamulin is an irreversible, highly selective inhibitior of human *CYP3Aa. Azamulin has CYP3A* inhibition activity with IC₅₀ values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .

HY-13463A

Avatrombopag maleate 5 Publications Verification AKR-501 maleate; E5501 maleate; YM477 maleate	Thrombopoietin Receptor Cytochrome P450 ERK STAT	Inflammation/Immunology Cancer
Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC₅₀: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .

HY-117789

Keto-itraconazole keto-ITZ	Cytochrome P450	Infection Cancer
Keto-itraconazole (keto-ITZ) is a metabolism of Itraconazole (HY-17514) with a potent inhibitor activity of *CYP3A. Keto-itraconazole shows unbound IC₅₀* value of 4.6 nM when coincubated with human liver microsomes and midazolam .

HY-13463B

Avatrombopag hydrochloride 5 Publications Verification AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride	Thrombopoietin Receptor	Cardiovascular Disease Cancer
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-100902

CDD3506	Cytochrome P450	Metabolic Disease
CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

HY-N7454

Anhydroerythromycin A	Drug Metabolite Bacterial	Infection
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.

HY-13463BS

Avatrombopag-d8 hydrochloride AKR-501-d8 hydrochloride; E5501-d8 hydrochloride; YM477-d8 hydrochloride	Isotope-Labeled Compounds Thrombopoietin Receptor	Cardiovascular Disease
Avatrombopag-d₈ (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-13463R

Avatrombopag (Standard) AKR-501 (Standard); E5501 (Standard); YM477 (Standard)	Reference Standards Thrombopoietin Receptor	Inflammation/Immunology Cancer
Avatrombopag (Standard) is the analytical standard of Avatrombopag. This product is intended for research and analytical applications. Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-A0069A

Doxylamine	Histamine Receptor Cytochrome P450	Neurological Disease Metabolic Disease
Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of *CYP2B, CYP2A, CYP3A* and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .

HY-B0696B

Tiagabine hydrochloride hydrate NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate	GABA Receptor	Neurological Disease
Tiagabine (NO050328; NO328; TGB) hydrochloride hydrate is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride hydrate exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride hydrate is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-A0069R

Doxylamine succinate (Standard)	Reference Standards Histamine Receptor Cytochrome P450	Neurological Disease Metabolic Disease
Doxylamine succinate (Standard) is the analytical standard of Doxylamine succinate (HY-A0069). This product is intended for research and analytical applications. Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of *CYP2B, CYP2A, CYP3A* and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .

HY-100901

CDD3505	Cytochrome P450	Metabolic Disease
CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

HY-N0693R

Schisandrin A (Standard) Schizandrin-A (Standard); Wuweizisu-A (Standard); Deoxyschizandrin (Standard)	Reference Standards Cytochrome P450 Autophagy Virus Protease	Inflammation/Immunology Cancer
Schisandrin A (Standard) is the analytical standard of Schisandrin A. This product is intended for research and analytical applications. Schisandrin A inhibits CYP3A activity with an IC₅₀ of 6.60 μM and Ki of 5.83 μM, respectively.

HY-135175

Phenoprolamine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Neurological Disease
Phenoprolamine hydrochloride is an adrenergic α1 receptor antagonist that exhibits potent antihypertensive effects. Phenoprolamine hydrochloride demonstrates neuroprotective and cardioprotective properties. Phenoprolamine hydrochloride inhibits CYP2D and CYP3A activities while down-regulating their mRNA transcription.

HY-N2621

Evodol	Cytochrome P450	Inflammation/Immunology
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitory activity against NO production . Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC₅₀ value of 32.43 μg/ml . Evodol has the inhibitory effect on CYP3A .

HY-N0692R

Schisandrol B (Standard) Gomisin-A (Standard); TJN-101 (Standard); Wuweizi alcohol-B (Standard)	Reference Standards Reactive Oxygen Species (ROS) Cytochrome P450 Autophagy	Cancer
Schisandrol B (Standard) is the analytical standard of Schisandrol B. This product is intended for research and analytical applications. Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities .

HY-13463BR

Avatrombopag hydrochloride (Standard) AKR-501 hydrochloride (Standard); E5501 hydrochloride (Standard); YM477 hydrochloride (Standard)	Thrombopoietin Receptor Reference Standards	Cardiovascular Disease Cancer
Avatrombopag (hydrochloride) (Standard) is the analytical standard of Avatrombopag (hydrochloride). This product is intended for research and analytical applications. Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-13463AR

Avatrombopag maleate (Standard) AKR-501 maleate (Standard); E5501 maleate (Standard); YM477 maleate (Standard)	Thrombopoietin Receptor Cytochrome P450 ERK STAT Reference Standards	Inflammation/Immunology Cancer
Avatrombopag (maleate) (Standard) is the analytical standard of Avatrombopag (maleate). This product is intended for research and analytical applications. Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-124626

(R)-(+)-Mequitazine	Histamine Receptor	Inflammation/Immunology
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .

HY-W110138

Chloroxoquinoline	DNA/RNA Synthesis Cytochrome P450 ROCK	Cancer
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on *CYP1A* and *CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity*, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .

HY-A0069AS

Doxylamine-d5	Isotope-Labeled Compounds Histamine Receptor Cytochrome P450	Neurological Disease Metabolic Disease
Doxylamine-d₅ is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of *CYP2B, CYP2A, CYP3A* and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .

HY-A0069S

Doxylamine-d5 succinate	Isotope-Labeled Compounds Histamine Receptor Cytochrome P450	Neurological Disease Metabolic Disease
Doxylamine-d₅ succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of *CYP2B, CYP2A, CYP3A* and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .

HY-B0696S

Tiagabine-d6 NO050328-d₆; NO328-d₆; TGB-d₆	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Tiagabine-d₆ (NO050328-d₆) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696AS

Tiagabine-d4 hydrochloride NO050328-d4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696AR

Tiagabine hydrochloride (Standard) NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-113327R

1,3,7-Trimethyluric acid (Standard)	Drug Metabolite Reference Standards Endogenous Metabolite	Cancer
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .

HY-179232

ERα antagonist 2	Estrogen Receptor/ERR	Cancer
ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

HY-100901R

CDD3505 (Standard)	Cytochrome P450 Reference Standards	Metabolic Disease
CDD3505 (Standard) is the analytical standard of CDD3505 (HY-100901). This product is intended for research and analytical applications. CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

HY-158252S

Tiagabine-d5 hydrochloride NO050328-d5 hydrochloride; NO328-d5 hydrochloride; TGB-d5 hydrochloride	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Tiagabine-d₅ (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696S1

Tiagabine-d4 NO050328-d₄; NO328-d₄; TGB-d₄	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Tiagabine-d₄ (NO050328-d₄) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by *CYP3A* and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

Cat. No.	Nombre del producto	Category	Target	Chemical Structure

HY-N0693

Schisandrin A 10+ Cited Publications Schizandrin-A; Wuweizisu-A; Deoxyschizandrin	Classification of Application Fields Lignans Phenylpropanoids Plants Schisandraceae Schisandra chinensis (Turcz.) Baill. Disease Research Fields Source Classification Cancer	Cytochrome P450 Autophagy Virus Protease
Schisandrin A inhibits *CYP3A* activity with an IC₅₀ of 6.60 μM and K_i of 5.83 μM, respectively.

HY-N0692

Schisandrol B 2 Publications Verification Gomisin-A; TJN-101; Wuweizi alcohol-B	Classification of Application Fields Lignans Phenylpropanoids Plants Schisandraceae Schisandra chinensis (Turcz.) Baill. Disease Research Fields Source Classification Cancer	Reactive Oxygen Species (ROS) Cytochrome P450 Autophagy
Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and *CYP3A* and also has anti-inflammatory, anti-diabetic and antioxidant activities .

HY-113327

1,3,7-Trimethyluric acid	Productos naturales Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Disease Research Fields Cancer Source Classification	Endogenous Metabolite
1,3,7-Trimethyluric acid is the metabolite of caffeine. The metabolic ratio 1,3,7-Trimethyluric acid to caffeine can be evaluated as a biomarker to describe variability in CYP3A activity in a cohort .

HY-N7454

Anhydroerythromycin A	Infection Structural Classification Macrolide Antibiotics Classification of Application Fields Antibiotics Antibacterial Disease Research Endogenous metabolite Disease Research Fields Source Classification	Drug Metabolite Bacterial
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.

HY-N0693R

Schisandrin A (Standard) Schizandrin-A (Standard); Wuweizisu-A (Standard); Deoxyschizandrin (Standard)	Structural Classification Lignans Phenylpropanoids Plants Schisandraceae Schisandra chinensis (Turcz.) Baill. Source Classification	Reference Standards Cytochrome P450 Autophagy Virus Protease
Schisandrin A (Standard) is the analytical standard of Schisandrin A. This product is intended for research and analytical applications. Schisandrin A inhibits CYP3A activity with an IC₅₀ of 6.60 μM and Ki of 5.83 μM, respectively.

HY-N2621

Evodol	Triterpenes Structural Classification Classification of Application Fields Terpenoids Evodia rutaecarpa (Juss.) Benth. Rutaceae Plants Inflammation/Immunology Disease Research Fields Source Classification	Cytochrome P450
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitory activity against NO production . Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC₅₀ value of 32.43 μg/ml . Evodol has the inhibitory effect on CYP3A .

HY-N0692R

Schisandrol B (Standard) Gomisin-A (Standard); TJN-101 (Standard); Wuweizi alcohol-B (Standard)	Structural Classification Lignans Phenylpropanoids Plants Schisandraceae Schisandra chinensis (Turcz.) Baill. Source Classification	Reference Standards Reactive Oxygen Species (ROS) Cytochrome P450 Autophagy
Schisandrol B (Standard) is the analytical standard of Schisandrol B. This product is intended for research and analytical applications. Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities .

HY-113327R

1,3,7-Trimethyluric acid (Standard)	Productos naturales Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Source Classification	Drug Metabolite Reference Standards Endogenous Metabolite
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .

Cat. No.	Nombre del producto	Chemical Structure

HY-13463BS

Avatrombopag-d8 hydrochloride

Avatrombopag-d₈ (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .

HY-A0069AS

Doxylamine-d5

Doxylamine-d₅ is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .

HY-A0069S

Doxylamine-d5 succinate

Doxylamine-d₅ succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .

HY-B0696S

Tiagabine-d6

Tiagabine-d₆ (NO050328-d₆) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696AS

Tiagabine-d4 hydrochloride

Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-158252S

Tiagabine-d5 hydrochloride

Tiagabine-d₅ (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696S1

Tiagabine-d4

Tiagabine-d₄ (NO050328-d₄) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

Cat. No.	Nombre del producto		Classification

HY-179232

ERα antagonist 2		Tetrazine
ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

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