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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
27 Results for "
CYP3A4 inhibition
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "CYP3A4 inhibition" in MCE Product Catalog:
1
Category:
Panax ginseng C. A. Meyer Triterpenes Terpenoids Plants Endogenous metabolite Disease Research Fields Araliaceae Cancer
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AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
Cat. No.: HY-157421
CAS No.: 2847156-05-0
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Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
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TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].
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YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
Cat. No.: HY-18569AR
CAS No.: 6505-45-9
Synonyms: Indole-3-acetic acid sodium (Standard); 3-IAA sodium (Standard)
Cat. No.: HY-W140208
CAS No.: 2404-87-7
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3-Phenylthiophene (Compound 25) is a CYP2A6 inhibitor with a Ki value of 3.3 μM. The Ki values for CYP2E1, CYP2B6, CYP2C9, and CYP2C19 are 9.7, 14, 112, and 107 μM respectively. It shows no significant inhibition on CYP3A4 and CYP2D6. 3-Phenylthiophene can be used in smoking cessation research .
Cat. No.: HY-131905S
CAS No.: 1606150-08-6
Cat. No.: HY-169217
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CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II) Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC50 of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min) .
Cat. No.: HY-N0598R
CAS No.: 53963-43-2
Synonyms: 20(S)-Ginsenoside F1 (Standard)
Cat. No.: HY-10779
CAS No.: 288079-93-6
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BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC50 = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC50 = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease .
Cat. No.: HY-130609
CAS No.: 2582757-69-3
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Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
Cat. No.: HY-180955
CAS No.: 773886-89-8
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Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a Ki value of 0.01 nM. Desfluoro-BMS-694153 has a significantly reduced risk of CYP3A4 inhibition, and its IC50 values for CYP3A4-BFC and CYP3A4-BZR are 36 and 6 μM respectively. Desfluoro-BMS-694153 can be used for research on migraines .
Cat. No.: HY-141547
CAS No.: 1432913-44-4
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Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain .
Cat. No.: HY-16641
CAS No.: 1315490-71-1
JAK1-IN-17 (Compound 31) is a highly selective inhibitor of JAK1 with a Ki of 1.9 nM. JAK1-IN-17 exhibits a low whole blood shift, which allows maintaining good whole blood potency. JAK1-IN-17 is also a nitrile-containing analogue with consistent, yet weak reversible inhibition of CYP3A4 using a midazolam probe (IC50 = 7.9 μM). JAK1-IN-17 can be studied in cancer research .
Cat. No.: HY-19397
CAS No.: 275375-69-4
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BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC50 = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K + efflux to hyperpolarize the cell membrane and reducing Ca 2+ influx. BMS-223131 can be used for the research of neurological disease, such as stroke .
Cat. No.: HY-175064
Synonyms: 3,4-MDPM hydrochloride
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3,4-Methylenedioxyphenmetrazine (3,4-MDPM) hydrochloride is a psychoactive substance. 3,4-Methylenedioxyphenmetrazine exhibits strong CYP2D6 inhibition and moderate inhibition of CYP3A4 and CYP1A2 .
Cat. No.: HY-121698
CAS No.: 1373353-95-7
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GW694481 is an ApoA1 upregulator with IC50 values of 2.1 μM for CYP2C9 inhibition and 17.0 μM for CYP3A4 inhibition. GW694481 upregulates ApoA1 expression in human hepatic cells.GW694481 can be used for the research of atherosclerosis .
Cat. No.: HY-L922
25000 compounds
A diverse compound library with favorable ADMET properties (Absorption, Distribution, Metabolism, Excretion, and Toxicity) is crucial in drug discovery. Early evaluation of ADMET properties allows for the exclusion of molecules with unfavorable profiles at the initial stages, thereby reducing the risk of late-stage development failures, lowering R&D costs, and accelerating optimization of lead compounds. Based on predictions from ADMET-related AI algorithms, the compounds in this library are predicted to exhibit favorable oral bioavailability (F > 30%), reasonable plasma protein binding (PPB < 98%), minimized CYP3A4 inhibition potential (inhibition probability < 50%, CYP3A4 is the most critical drug-metabolizing enzyme in the cytochrome P450 family) , low toxicity profiles, with 140 potentially toxic substructures pre-identified and excluded via substructure searching to eliminate compounds containing hazardous fragments. The diversity library enables broad applicability in high-throughput screening (HTS) and high-content screening (HCS).
Cat. No.: HY-123965
CAS No.: 2089334-01-8
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PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC50 of 0.4 nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
