101 Results for "

Plasma Stability

" in MedChemExpress (MCE) Product Catalog:
Products (101)

101 Results for "Plasma Stability" in MCE Product Catalog:

Cat. No.: HY-P1615
CAS No.: 1006388-38-0
Synonyms: UPARANT
Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases .
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Cat. No.: HY-153715
CAS No.: 866465-21-6
Purity:  ≥95.0%
Synonyms: Mitochondria modulator-1
Research Areas:  

Metabolic Disease

NV-354 (Mitochondria modulator-1) (compound 1) is a mitochondrial regulator that stimulates mitochondrial ATP production. NV-354 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. NV-354 has the potential to study mitochondrial diseases .
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Cat. No.: HY-159563
CAS No.: 2778229-31-3
Research Areas:  

Cancer

Mal-va-mac-SN38 is a drug-linker conjugate for ADC. Mal-va-mac-SN38 contains a ADC cytotoxin SN-38 (HY-13704) and a linker (HY-126364). Mal-va-mac-SN38 can rapidly and covalently bind with endogenous albumin in vivo, resulting in the formation of HSA-va-mac-SN38. Mal-va-mac-SN38 demonstrates exceptional stability in human plasma, and has anti-tumor and anti-metastasis effect .
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Cat. No.: HY-143255
CAS No.: 2631703-04-1
Research Areas:  

Cancer

Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
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Cat. No.: HY-117187
CAS No.: 421580-53-2
Target:  

CFTR

Research Areas:  

Others

Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein .
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Cat. No.: HY-144772
CAS No.: 1580-42-3
Target:  

SARS-CoV

Research Areas:  

Infection

SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
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Cat. No.: HY-164429
CAS No.: 2418533-90-9
Target:  

Integrin Elastase

Research Areas:  

Cancer

VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
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Cat. No.: HY-169323
CAS No.: 2921735-87-5
Synonyms: Mal-Exo-EEVC-MMAE
Research Areas:  

Cancer

APL-1091 (Mal-Exo-EEVC-MMAE) is an ADC payload-linker conjugate (Drug-Linker Conjugates for ADC). APL-1091 is formed by the conjugation of the Mal-Exo-EEVC (HY-169353) linker and MMAE (HY-15162), a microtubule inhibitor. APL-1091 resists aggregation at high drug-to-antibody ratio (DAR), exhibits excellent plasma stability, and reduces premature payload release. When conjugated with Trastuzumab (HY-P9907), APL-1091 displays anti-tumor activity in gastric cancer xenograft models. APL-1091 can be used for ADC synthesis and gastric cancer-related research .
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Cat. No.: HY-13611
CAS No.: 220997-97-7
Synonyms: BN 80915
Target:  

Topoisomerase

Research Areas:  

Cancer

Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
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Cat. No.: HY-112913
CAS No.: 2169316-15-6
Purity:  99.73%
Target:  

CRAC Channel

SOCE inhibitor 1 (Compound 39) is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM. SOCE inhibitor 1 has a good stability in plasma .
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Cat. No.: HY-170546
CAS No.: 3067968-52-6
Target:  

Haspin Kinase

Research Areas:  

Cancer

MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
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Cat. No.: HY-175818
Target:  

Apelin Receptor (APJ)

Research Areas:  

Cancer

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis .
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Cat. No.: HY-144770
CAS No.: 56961-10-5
Purity:  98.90%
Target:  

SARS-CoV

Research Areas:  

Infection

SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
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Cat. No.: HY-170509
Ferroptosis-IN-17 (Compound 18) is a ferroptosis (Ferroptosis) inhibitor with an EC50 value of 0.57 μM. Ferroptosis-IN-17 reduces intracellular ferrous ion accumulation, lipid peroxidation, and effectively restores the levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). Ferroptosis-IN-17 shows good solubility and significant metabolic stability in rat plasma. Ferroptosis-IN-17 is promising for research in tumor suppression, neurodegenerative diseases, and cardiovascular diseases .
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Cat. No.: HY-P2161
CAS No.: 872719-49-8
Target:  

Kisspeptin Receptor

Research Areas:  

Cancer

TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
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Cat. No.: HY-178794
CAS No.: 3038861-75-2
Target:  

PGE synthase

Research Areas:  

Inflammation/Immunology

AGU661 is a Microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with an IC50 of 0.22  nM. AGU661 lowers PGE2 formation in human pro-inflammatory M1 macrophages and activated monocytes without affecting other lipid mediator pathways. AGU661 has unfavorable physicochemical properties with poor metabolic stability and strong plasma protein binding tendencies. AGU661 into PLGA-based NPs significantly enhances its bioactivity. AGU661 can be used for inflammatory disorders research .
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Cat. No.: HY-163783
CAS No.: 3105428-74-5
Target:  

Casein Kinase

Research Areas:  

Infection

CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
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Cat. No.: HY-W099504S
CAS No.: 194793-95-8
Synonyms: n-Heptyl alcohol-d15
n-Heptyl Alcohol-d15 is the deuterium labeled 1-Heptanol. 1-Heptanol (n-Heptyl alcohol) is a linear primary fatty alcohol. 1-Heptanol selectively inhibits the activating phosphorylation of SAPK/JNK and reduces the phosphorylation level of IκB-α. 1-Heptanol increases plasma membrane fluidity, decreases membrane thermal stability, alters the coupling kinetics of STIM1-ORAI1, inhibits the production of ROS and LTC4, and induces the expression of HSP70. 1-Heptanol is used in the fragrance industry due to its pleasant odor .
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Cat. No.: HY-P6053
CAS No.: 2775287-98-2
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
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Cat. No.: HY-160031
CAS No.: 2765065-09-4
Target:  

GLP Receptor

Research Areas:  

Cardiovascular Disease

GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
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