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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
42 Results for "
high exposure
" in MedChemExpress (MCE) Product Catalog:
Products (42)
42 Results for "high exposure" in MCE Product Catalog:
3
Category:
Quinones other families Other Diseases Plants Disease Research Fields Naphthalene Quinones Pteris livida Mett.
Target:
2
2 Cited Publications
Research Areas:
Necrocide 1, a necrosis by sodium overload (NECSO) inducer, is a selective transient receptor potential melastatin 4 (TRPM4) agonist with an EC50 of 306.3 nM for human TRPM4. Necrocide 1 triggers TRPM4-dependent necrotic cell death through the induction of sodium influx. Necrocide 1 induces hallmarks of immunogenic cell death incurring calreticulin (CALR) exposure, ATP secretion and high mobility group box 1 (HMGB1) release. Necrocide 1 can be used for the study of breast and prostate cancer .
1
Target:
Synonyms: ABSK011
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
Cat. No.: HY-W099594
CAS No.: 7281-04-1
Synonyms: Benzyldimethyldodecylammonium bromide
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ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
Cat. No.: HY-163087
CAS No.: 3037561-48-8
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PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
Cat. No.: HY-W116007
CAS No.: 556-67-2
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Octamethylcyclotetrasiloxane promotes the anchorage-independent growth of MCF-10A and MCF-10F cells. Octamethylcyclotetrasiloxane induces DNA damage, inhibits the expression of DNA-repairing protein BRCA1 under long-term and high-concentration exposure. Octamethylcyclotetrasiloxane exhibits intrinsic estrogenic activity .
Cat. No.: HY-175728
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VU6032735 is a potent and subtype-selective sperm-specific potassium channel 3 (SLO3) inhibitor with IC50 values of 165 nM (hSLO3) and 730 nM (mSLO3). VU6032735 also inhibits sodium channel and L-type calcium channel VU6032735 can sustain high tissue exposure in the fertilized oviduct. VU6032735 can be used for the research of contraception .
Synonyms: 2-Amino-α-carboline; AαC
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AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
Synonyms: BY-108330
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Spirotetramat (BY-108330) is an orally active Insecticide and lipid biosynthesis inhibitor. Spirotetramat regulates the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), with short-term exposure increasing their activities and long-term exposure altering their activities. Spirotetramat induces the activity and mRNA expression of carboxylesterase (CarE). Spirotetramat induces oxidative stress and lipid peroxidation in tadpoles. Spirotetramat is toxic to amphibian tadpoles and exhibits sublethal/non-lethal toxicity to amphibians. Spirotetramat causes death in immature psyllids, aphids, scale insects, mealybugs, whiteflies and thrips, and shows a high lethal rate against Cacopsylla pyri nymphs. Spirotetramat reduces the fecundity of Aphis gossypii. Spirotetramat induces tolerance in the offspring of exposed Aphis gossypii, and acts on Myzus persicae, Bemisia tabaci and Tetranychus urticae .
Cat. No.: HY-14375
CAS No.: 289715-28-2
CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft . CB 300919 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-125920R
CAS No.: 137-16-6
Synonyms: Sarkosyl NL sodium (Standard)
Synonyms: (1S,5R)-CP-601927
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CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
Cat. No.: HY-130609A
CAS No.: 2434633-17-5
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Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 μM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease .
Cat. No.: HY-130609
CAS No.: 2582757-69-3
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Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
Cat. No.: HY-157455
CAS No.: 2902679-53-0
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AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
Cat. No.: HY-156593
CAS No.: 2643334-76-1
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
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WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
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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
