Cytochrome P450 Inhibitor

1-Ethynylnaphthalene (Standard) is the analytical standard of 1-Ethynylnaphthalene (HY-111430). This product is intended for research and analytical applications. 1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. 1-Ethynylnaphthalene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Org 33201 is an orally active and selective Aromatase inhibitor with an IC₅₀ of 2.2 nM. Org 33201 inhibits the activity of Aromatase by binding to its heme iron. Org 33201 can be used in the study of estrogen-dependent diseases (such as postmenopausal breast cancer).

KBP-7018 is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC₅₀ value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 can be used in research related to idiopathic pulmonary fibrosis.

NNC 55-0396 free base is a blood-brain-barrier-permeable T-type Ca²⁺ channel inhibitor and pan-P450 inhibitor. NNC 55-0396 free base selectively inhibits T-type Ca²⁺ channels, suppresses HIF-1α expression and stability and inhibits Kv currents. NNC 55-0396 free base reduces brain infarct and attenuates neurological dysfunction. NNC 55-0396 free base inhibits the activity of multiple P450 enzymes. NNC 55-0396 (free base) can be used for the research of brain injury, hypertension, and glioblastoma.

Paroxetine-d₄ (BRL29060-d₄) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research.

2-(3-Pyridyl)-benzimidazole is an Aminopyrine N-Demethylase inhibitor.

DMU2105 (Standard) is the analytical standard of DMU2105 (HY-101284). This product is intended for research and analytical applications. DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.

21-Hydroxypregnenolone (Standard) is the analytical standard of 21-Hydroxypregnenolone (HY-113020). This product is intended for research and analytical applications. 21-Hydroxypregnenolone is a CYP17 inhibitor. 21-Hydroxypregnenolone competitively inhibits CYP17-mediated 17α-hydroxylation activity of progesterone, with a Ki value of 36.4 μM.

SU-8000 is an inhibitor that selectively targets 17α-hydroxylase and C_17-20-lyase in rat testes. When administered to pregnant rats, SU-8000 can cause hypospadias in male fetuses.

Pipercroside A is found in Piper crocatum Ruiz & Pav. Pipercroside A is a CYP51 inhibitor. Pipercroside A has antifungal activity.

Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC₅₀=25.60 μM) properties.

GW844520 is an orally active inhibitor of cytochrome bc1 complex. GW844520 can be used in malaria and anti-plasmodium related research.

DMU2139 (Standard) is the analytical standard of DMU2139 (HY-101285). This product is intended for research and analytical applications. DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca²⁺-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme.

Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.

2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109). Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.

Feruloylputrescine is an oral active phenolamide found in citrus plants and formed through the decarboxylation of L-Arginine. Feruloylputrescine inhibits monooxygenase (cntA) and reductase (cntB) and trimethylamine production. Feruloylputrescine can be used for cardiovascular diseases research.

NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC₅₀ values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1.