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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
1014 Results for "
Bioavailability
" in MedChemExpress (MCE) Product Catalog:
Products (1014)
1014 Results for "Bioavailability" in MCE Product Catalog:
Cat. No.: HY-173024
CAS No.: 3053390-98-7
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TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
Cat. No.: HY-173032
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VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
Cat. No.: HY-173235
CAS No.: 2604662-64-6
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Galectin-3-IN-6 is a human and murine galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM against human galectin-3, an IC50 of 12.6 nM against mutant murine galectin-3 (V160A), and a Kd of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis .
Cat. No.: HY-176221
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α-Glucosidase-IN-92 (compound 14b) is a non-competitive inhibitor targeting α-glucosidase (IC50=64.0 μM), with better inhibitory potency than Acarbose (HY-B0089) (IC50=750 μM). α-Glucosidase-IN-92 has good oral bioavailability and can cross the blood-brain barrier. α-Glucosidase-IN-92 can delay carbohydrate hydrolysis and reduce postprandial blood glucose. α-Glucosidase-IN-92 can be used in anti-glycemic research for type 2 diabetes .
Cat. No.: HY-176533
CAS No.: 3107268-28-7
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S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC50 of 85.4 nM and human S1PR5 Kd of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis .
Cat. No.: HY-181611
CAS No.: 3068829-46-6
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Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers .
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease .
Cat. No.: HY-10672
CAS No.: 1034708-07-0
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Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
Synonyms: Ro 24-7375
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Cat. No.: HY-111790R
CAS No.: 2285330-15-4
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M3258 (Standard) is the analytical standard of M3258 (HY-111790). This product is intended for research and analytical applications. M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
Cat. No.: HY-112306R
CAS No.: 1442472-39-0
Synonyms: DCC-2618 (Standard)
Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
Cat. No.: HY-12169R
CAS No.: 154039-60-8
Synonyms: BB2516 (Standard); TA2516 (Standard)
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Marimastat (Standard) is the analytical standard of Marimastat. This product is intended for research and analytical applications. Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes .
Synonyms: S/GSK1349572-d3
Cat. No.: HY-13238S2
CAS No.: 2249814-82-0
Synonyms: S/GSK1349572-d5
Cat. No.: HY-13270A
CAS No.: 141450-48-8
Synonyms: E7010 hydrochloride
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ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
Cat. No.: HY-15007
CAS No.: 138382-23-7
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L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists .
Cat. No.: HY-162484
CAS No.: 3089845-68-8
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GZNL-P36 is an orally active inhibitor for SARS-CoV-2 papain-like protease (PL pro), with an IC50 of 6.45 nM. GZNL-P36 inhibits SARS-CoV and its variants with EC50 range from 58.2 nM to 2.66 μM. GZNL-P36 exhibits a peak plasma concentration Cmax of 549 ng/mL, a half-life T1/2 of 1.45 h and a bioavailability of 74.7% in CD-1 mouse. GZNL-P36 exhibits antiviral activity in SARS-CoV-2 XXB.1 infection in mouse .
Cat. No.: HY-173059
CAS No.: 3029608-57-6
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
Cat. No.: HY-189008
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17β-HSD13-IN-1 is a selective 17β-HSD13 inhibitor with a human IC50 of 9 nM, high selectivity over 17β-HSD1, nanomolar cellular activity, broad pH solubility, extended rodent plasma mean residence times, and high oral bioavailability in Mus musculus. 17β-HSD13-IN-1 engages in hydrophobic interactions with specific active-site amino acids of its target enzyme. 17β-HSD13-IN-1 can be used for the research of metabolic dysfunction-associated steatohepatitis (mash) .
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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
