2. Search Result
Search Result
Results for "

In vitro stability

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

2

Fluorescent Dye

1

Natural
Products

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163350
    TUG-2208

    		GPR84 Inflammation/Immunology
    TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability .
    TUG-2208
  • HY-W419570
    (Rac)-BX 048

    		P2Y Receptor Cardiovascular Disease
    (Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
    (Rac)-BX 048
  • HY-16750
    Radalbuvir

    GS-9669

    		 HCV Infection
    Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM) .
    Radalbuvir
  • HY-156188
    AChE-IN-41

    		Cholinesterase (ChE) Others
    AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
    AChE-IN-41
  • HY-119324
    Anticancer agent 254

    		Apoptosis Others
    Anticancer agent 254 (compound 10) is a dichloroacetic acid-loaded compound with enhanced antitumor activity against leukemia cells in vitro and better stability in vivo, and can be considered for preclinical evaluation of cancer inhibition.
    Anticancer agent 254
  • HY-D2334
    AlF-NOTA-c-d-VAP

    		Radionuclide-Drug Conjugates (RDCs) HSP Cancer
    AlF-NOTA-c-d-VAP is a peptide positron emission tomography (PET) probe that used for targeted tumor imaging of GRP78. AlF-NOTA-c-d-VAP demonstrates high stability in vitro and in vivo .
    AlF-NOTA-c-d-VAP
  • HY-155813
    MPI60

    		SARS-CoV Infection
    MPI60 is a potent SARS-CoV-2 M Pro inhibitor with high antiviral potency, low cellular cytotoxicity, and high in vitro metabolic stability. MPI60 can be used for SARS-CoV-2 research .
    MPI60
  • HY-15980
    GNF179 (Metabolite)

    		Parasite Infection
    GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
    GNF179 (Metabolite)
  • HY-174440
    BWD

    		PSMA Cancer
    BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research .
    BWD
  • HY-152469
    Eleven-Nineteen-Leukemia Protein IN-1

    		Epigenetic Reader Domain Cancer
    Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro .
    Eleven-Nineteen-Leukemia Protein IN-1
  • HY-120391
    LiLo

    		Biochemical Assay Reagents Others
    LiLo is a new bifunctional chelator that has the activity of forming kinetically stable chelates with metal ions (such as indium). After using LiLo to bind indium-111 to monoclonal antibodies, the in vitro stability and in vivo biodistribution of the conjugates are superior to those using other chelators.
    LiLo
  • HY-147950
    PDE4-IN-10

    		Phosphodiesterase (PDE) TNF Receptor Inflammation/Immunology
    PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro .
    PDE4-IN-10
  • HY-119002
    BO-1236

    		Antibiotic Others
    BO-1236 is a compound with antibacterial activity. It has strong activity against Gram-negative bacteria including Pseudomonas aeruginosa. It has shown activity superior to or equivalent to that of some commonly used antibiotics in in vitro and in vivo experiments, and has a certain stability against β-lactamase.
    BO-1236
  • HY-173623
    EU 1622-240

    		iGluR Neurological Disease
    EU 1622-240 is a biased positive allosteric modulator of GluN2B, GluN2C, and GluN2D, with EC50s of 0.57, 0.82, 1.1 μM respectively. EU 1622-240 has good physicochemical properties, in vitro stability, and permeability .
    EU 1622-240
  • HY-152471
    Eleven-Nineteen-Leukemia Protein IN-3

    		Epigenetic Reader Domain Cancer
    Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro .
    Eleven-Nineteen-Leukemia Protein IN-3
  • HY-175413
    FTAC6

    		Biochemical Assay Reagents Others
    FTAC6 (C6F-TAC) is a lipophobic surfactant. FTAC6 does not solubilize biological membranes as a non-detergent and can substitute for detergents to keep membrane proteins soluble and improves stability after conventional solubilization. FTAC6 can be utilized in in vitro synthesis of membrane proteins .
    FTAC6
  • HY-156093
    TPH1-IN-1

    		Tryptophan Hydroxylase Metabolic Disease
    TPH1-IN-1 (compound 40) is a xanthine derivative and an inhibitor of tryptophan hydroxylase TPH1 (IC50: 110.1 nM). TPH1-IN-1 has good in vitro activity and liver microsome stability, and effectively inhibits adipocyte differentiation of T3-L1 cells .
    TPH1-IN-1
  • HY-128947
    CL2 Linker

    		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) .
    CL2 Linker
  • HY-160656
    5-HT/NA Reuptake inhibitor-1

    		5-HT Receptor Neurological Disease
    5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
    5-HT/NA Reuptake inhibitor-1
  • HY-146248
    TFMU-ADPr

    		Poly(ADP-ribose) Glycohydrolase (PARG) Others
    TFMU-ADPr is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr has excellent reactivity, generality, stability, and usability. TFMU-ADPr is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes .
    TFMU-ADPr
  • HY-149920
    Anticancer agent 98

    		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 .
    Anticancer agent 98
  • HY-152468
    Antitumor agent-83

    		Apoptosis Cancer
    Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
    Antitumor agent-83
  • HY-168930
    ATX inhibitor 25

    		Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. ATX inhibitor 25 exhibits excellent in vitro metabolic stability, with a t1/2 of more than 170 minutes. In the bleomycin (HY-108345)-induced pulmonary fibrosis mouse model, orally administered ATX inhibitor 25 shows anti-fibrotic effects .
    ATX inhibitor 25
  • HY-122229
    GS-9822

    		HIV Infection
    GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
    GS-9822
  • HY-155687
    PDE5-IN-10

    		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 .
    PDE5-IN-10
  • HY-169429
    CHIKV-IN-5

    		Flavivirus Infection
    CHIKV-IN-5 (Compound 26) is a CHIKV inhibitor (EC90 = 0.45 μM). CHIKV-IN-5 inhibits CHIKV replication at a late stage in the virus life cycle by blocking structural protein translation. CHIKV-IN-5 has great in vitro mouse microsomal stability. CHIKV-IN-5 reduces footpad swelling and decreases virus dissemination to other tissues in mice infected with CHIKV .
    CHIKV-IN-5
  • HY-146248A
    TFMU-ADPr triethylamine

    		Poly(ADP-ribose) Glycohydrolase (PARG) Others
    TFMU-ADPr triethylamine is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr triethylamine can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr triethylamine has excellent reactivity, generality, stability, and usability. TFMU-ADPr triethylamine is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes .
    TFMU-ADPr triethylamine
  • HY-174375
    NEDD4-IN-1

    		Others Cancer
    NEDD4-IN-1 (Compound 32) is a potent inhibitor of NEDD4 (IC50 = 0.12 μM). NEDD4-IN-1 shows significant and comparable antiproliferative activity in H292 cell line. NEDD4-IN-1 demonstrates high plasma protein binding and medium-to-high in vitro clearance in both human and mouse models. NEDD4-IN-1 shows superior stability in mouse plasma. NEDD4-IN-1 has excellent potency, selectivity, and favourable in vitro ADME properties. NEDD4-IN-1 exhibits a systemic plasma clearance exceeding the hepatic blood flow in mouse model. NEDD4-IN-1 can be studied in anticancer research .
    NEDD4-IN-1
  • HY-138648
    PB1

    		ERK Neurological Disease
    PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
    PB1
  • HY-146018
    HIV-1 inhibitor-23

    		HIV Infection
    HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability .
    HIV-1 inhibitor-23
  • HY-174413
    A2AAR antagonist 3

    		Adenosine Receptor Cancer
    A2AAR antagonist 3 is a selective and potent A2A adenosine receptor (A2A AR) antagonist with an IC50 of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
    A2AAR antagonist 3
  • HY-169064
    HIV-1 inhibitor-75

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes .
    HIV-1 inhibitor-75
  • HY-131445A
    SS-RJW100

    		Orphan Receptor Metabolic Disease Inflammation/Immunology
    SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability .
    SS-RJW100
  • HY-156654
    Ibuzatrelvir

    PF-07817883

    		 SARS-CoV Virus Protease Infection
    Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
    Ibuzatrelvir
  • HY-162600
    CDK8-IN-15

    		CDK Inflammation/Immunology
    CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases .
    CDK8-IN-15
  • HY-112766
    DPyPE

    		Liposome Others
    DPyPE is a neutral phosphatidylethanolamine lipid composed of a polyisoprene alkyl chain with two pyridine-containing phosphine ligands. DPyPE is mainly used in liposome formulations and to enhance the efficiency of gene delivery in vitro and in vivo. For example, DPyPE can be mixed with cationic lipids such as VC1052 (HY-156616) (in a 1:1 ratio) to form the vaccine adjuvant Vaxfectin (HY-142998). DPyPE assists VC1052 in binding to negatively charged pDNA to form a uniform liposome complex by regulating the fluidity and stability of the liposome membrane .
    DPyPE
  • HY-170887
    MAO-B-IN-39

    		Keap1-Nrf2 Monoamine Oxidase Inflammation/Immunology
    MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC50 of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research .
    MAO-B-IN-39
  • HY-155732
    NPD-2975

    		Parasite Infection
    NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
    NPD-2975
  • HY-121081
    BAY-958

    		CDK Cancer
    BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
    BAY-958
  • HY-N10159
    1-Benzyl-I3C

    		Others Cancer
    1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1 .
    1-Benzyl-I3C

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: