Search Result
Results for "
t1/2
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-118770
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K 5407 free base
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Adrenergic Receptor
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Cardiovascular Disease
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Nafetolol (K 5407), specifically effective on cardiac (β1)-adrenoceptors, is an orally active β blocking agent, with a t1/2 of ~ 2 h in dogs [1].
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- HY-153822
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Tau Protein
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Neurological Disease
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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].
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- HY-162655
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Others
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Neurological Disease
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SLF80821178 is a potent and orally active inhibitor of Sphingosine-1-Phosphate Transporter (Spns2). SLF80821178 inhibits S1P release with an IC50 of 51 nM in HeLa cells and a T1/2 of 2.4 h in mouse [1].
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- HY-145362
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LPL Receptor
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Others
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S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
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- HY-16309
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Phosphatase
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Metabolic Disease
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MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
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- HY-P10219
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Bacterial
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Infection
Inflammation/Immunology
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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].
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- HY-113567
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FXR
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Metabolic Disease
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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].
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- HY-100866B
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Bcl-2 Family
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Cancer
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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].
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- HY-100866
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Bcl-2 Family
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Cancer
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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].
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- HY-139721
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HIV
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Infection
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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.
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- HY-100866A
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Bcl-2 Family
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Cancer
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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].
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- HY-162406
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TAM Receptor
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Cancer
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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].
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- HY-159489
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SHP2
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Cancer
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SDUY038 is a SHP2 allosteric inhibitor, with an IC50 of 1.2 μM and KD of 0.29 μM, respectively. SDUY038 exhibits pan-antitumor activity (IC50 = 7-24 μM) by suppressing pERK expression. SDUY038 exhibits t1/2 of 3.95 h by oral administration [1].
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- HY-128947
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ADC Linker
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Cancer
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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] .
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- HY-146054
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CXCR
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Inflammation/Immunology
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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].
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- HY-162408
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Protease Activated Receptor (PAR)
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Others
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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].
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- HY-162409
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Protease Activated Receptor (PAR)
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Others
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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].
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- HY-158090
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Others
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Cancer
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Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier [1].
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- HY-118717
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mTOR
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Cancer
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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].
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- HY-155687
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Phosphodiesterase (PDE)
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Neurological Disease
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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].
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- HY-146594
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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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].
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- HY-15990
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HSP
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Cancer
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CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy [1].
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- HY-139722
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HIV
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Infection
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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.
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- HY-146034
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NOD-like Receptor (NLR)
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Inflammation/Immunology
Cancer
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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].
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- HY-148571
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- HY-157334
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Molecular Glues
Casein Kinase
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Cancer
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DEG-77, a IKZF2 and CK1α targeted molecular glue, possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t1/2=8h) .
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- HY-155051
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Apoptosis
Histone Methyltransferase
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Cancer
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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].
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- HY-162484
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SARS-CoV
Virus Protease
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Infection
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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 [1].
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- HY-155050
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Apoptosis
Histone Methyltransferase
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Cancer
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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].
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- HY-N12728
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Others
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Others
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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].
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- HY-149920
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Microtubule/Tubulin
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Cancer
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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].
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- HY-155354
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Parasite
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Infection
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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 .
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- HY-149663
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Acyltransferase
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Metabolic Disease
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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 .
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- HY-N6720
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Endogenous Metabolite
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Metabolic Disease
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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 .
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- HY-162583
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
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- HY-163345
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5-HT Receptor
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Neurological Disease
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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 |
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- HY-149916
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Adenosine Receptor
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Cancer
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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) .
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- HY-113338A
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Endogenous Metabolite
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Others
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8-Hydroxyguanine hydrochloride is a DNA damage product under oxidative stress, which is formed when hydroxyl radicals attack guanine in DNA. 8-Hydroxyguanine hydrochloride induces mutagenesis and leads to a transversion from G to T .
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- HY-153456
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Hedgehog
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Cancer
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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].
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- HY-143400
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HSP
Hedgehog
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Cancer
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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].
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- HY-108568
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15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2
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PPAR
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
Cancer
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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] .
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- HY-108568S
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15d-PGJ2-d4; 15-Deoxy-Δ12,14-PGJ2-d4
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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].
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- HY-108568R
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PPAR
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
Cancer
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15-Deoxy-Δ-12,14-prostaglandin J2 (Standard) is the analytical standard of 15-Deoxy-Δ-12,14-prostaglandin J2. This product is intended for research and analytical applications. 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] .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10219
-
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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].
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- HY-100866B
-
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Bcl-2 Family
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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].
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- HY-100866
-
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Bcl-2 Family
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Cancer
|
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].
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- HY-100866A
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Bcl-2 Family
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Cancer
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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].
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-108568S
-
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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].
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