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Results for "

t1/2

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

4

Peptides

3

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153822

    Tau Protein Neurological Disease
    JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays [1].
    JG-23
  • HY-145362

    LPL Receptor Others
    S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
    S1P1 agonist 4
  • HY-P10219

    Bacterial Infection Inflammation/Immunology
    Brevicidine analog 22 (22) exerts broad spectrum antimicrobial activity and excellent stability (t1/2 = 40.98 h), with MICs of 2-16 μM for gram-negative and gram-positive bacteria [1].
    Brevicidine analog 22
  • HY-113567

    FXR Metabolic Disease
    GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively [1].
    GSK2324
  • HY-100866B

    Bcl-2 Family Cancer
    F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI [1].
    F1324 acetate
  • HY-100866

    F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI [1].
    F1324
  • HY-139721

    HIV Infection
    Tenofovir-C3-O-C15-CF3 (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
    Tenofovir-C3-O-C15-CF3 ammonium
  • HY-100866A

    Bcl-2 Family Cancer
    F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI [1].
    F1324 TFA
  • HY-162406

    Others Cancer
    UNC8969 (compound 43) is a MERTK/AXL dual inhibitor with IC50s of 1.1±0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. UNC8969 also exerts a T1/2 of 7.3 h with 5 mg/kg i.v. in mice [1].
    UNC8969
  • HY-128947

    ADC Linker Cancer
    CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in agent substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours) [1] .
    CL2 Linker
  • HY-146054

    CXCR Inflammation/Immunology
    CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model [1].
    CXCR4 modulator-2
  • HY-162408

    Protease Activated Receptor (PAR) Others
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min [1].
    PAR4 antagonist 3
  • HY-162409

    Protease Activated Receptor (PAR) Others
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min [1].
    PAR4 antagonist 4
  • HY-158055

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-20 (Compound ZC9) is an inhibitor for Keap-Nrf2 pathway with KD2 of 51 nM. Keap1-Nrf2-IN-20 exhibits good cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h) [1].
    Keap1-Nrf2-IN-20
  • HY-118717

    mTOR Cancer
    mTOR inhibitor WYE-28 (compound 28) is a selective inhibitor of mTOR>/b< (IC50)=0.08 nM. mTOR inhibitor WYE-28 inhibits PI3Kα with an IC50 value of 6 nM. mTOR inhibitor WYE-28 shows a metabolic time (T1/2) in nude mouse microsomes of 13 min [1].
    mTOR inhibitor WYE-28
  • HY-155687

    Phosphodiesterase (PDE) Neurological Disease
    PDE5-IN-10 (compound 4b) is a potent PDE5 inhibitor with an IC50 of 20 nM. PDE5-IN-10 improves in vitro microsomal stability (t1/2 = 44.6 min) as well as excellent efficacy in restoring long-term potentiation. PDE5-IN-10 can be used for Alzheimer’s disease (AD) research [1].
    PDE5-IN-10
  • HY-146594

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM) [1].
    NLRP3-IN-8
  • HY-139722

    HIV Infection
    Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo. Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
  • HY-146034

    NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) [1].
    NOD1/2 antagonist-1
  • HY-148571

    MMP Inflammation/Immunology Cancer
    TP0597850 is a selective inhibitor of MMP2 (IC50=0.22 nM). TP0597850 has a long MMP2 dissociation half-life (t1/2=265 min) .
    TP0597850
  • HY-157334

    Casein Kinase Cancer
    DEG-77, a PROTAC based IKZF2 and CK1α degrader, possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t1/2=8h) .
    DEG-77
  • HY-155051

    Apoptosis Histone Methyltransferase Cancer
    Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes [1].
    Antiproliferative agent-25
  • HY-155050

    Apoptosis Histone Methyltransferase Cancer
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) [1].
    PRMT5-IN-31
  • HY-N12728

    Others Others
    Heteroclitin G is a lignan which can be extracted from Dian-Jixueteng. Heteroclitin G (2.0 mg/kg, i.v.) exerts an C5min of 665.97 ± 29.89 ng/mL and T1/2z of 5.04 ± 1.84 h [1].
    Heteroclitin G
  • HY-149920

    Microtubule/Tubulin Cancer
    Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min [1].
    Anticancer agent 98
  • HY-155354

    Parasite Infection
    Antimalarial agent 33 (compound 5g) has antiplasmodial activity against erythrocytic and hepatic stages of Plasmodium with an EC50 of 1.1 μM for K1 P. falciparum strain. Antimalarial agent 33 demonstrats enhanced microsomal stability (T1/2=29 min). Antimalarial agent 33 has no significant cytotoxicity against primary hepatocytes .
    Antimalarial agent 33
  • HY-149663

    Acyltransferase Metabolic Disease
    BMS-986172 is an orally active, highly selective MGAT2 inhibitor with an IC50 of 4.6 nM and 20 nM for hMGAT2 and mMGAT2, respectively. BMS-986172 has a T1/2>120 min in vitro assays. BMS-986172 reduces food intake and body weight. BMS-986172 has the potential for metabolic disorders such as obesity and NASH research .
    BMS-986172
  • HY-N6720

    Endogenous Metabolite Metabolic Disease
    T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin [1]. T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively .
    T-2 Triol
  • HY-163345

    5-HT Receptor Neurological Disease
    5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment [1].
    Pharmacokinetic Analysis ICR Male Mice [1]

    药代动力学分析 [1]
    Plasma Intravenous Administration Intraperitoneal Administration
    Tmax (h) 0.08 0.25
    T1/2 (h) 0.77 1.06
    Cmax (ng/mL) 33.07 156.44
    AUClast (ng·h/mL) 28.31 143.27
    CL (L/h/kg) 41.61 -
    Vss (L/kg) 32.43 -
    MRT (h) 0.79 0.93
    F (%) 50.60
    5-HT7R antagonist 2
  • HY-149916

    Adenosine Receptor Cancer
    A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
    A2AR-antagonist-1
  • HY-153456

    Hedgehog Cancer
    Hedgehog IN-2 (Compound 20) is an inhibitor of Hedgehog pathway with an IC50 value less than 0.003 μM in C3H10T1/2 cells [1].
    Hedgehog IN-2
  • HY-143400

    HSP Hedgehog Cancer
    HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 [1].
    HSP70-IN-3
  • HY-108568
    15-Deoxy-Δ-12,14-prostaglandin J2
    1 Publications Verification

    15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2

    PPAR Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM [1] .
    15-Deoxy-Δ-12,14-prostaglandin J2
  • HY-108568S

    15d-PGJ2-d4; 15-Deoxy-Δ12,14-PGJ2-d4

    PPAR Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
    15-Deoxy-Δ-12,14-prostaglandin J2-d4

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