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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
35 Results for "
whole-cell
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "whole-cell" in MCE Product Catalog:
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Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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2 Cited Publications
Cat. No.: HY-W134422
CAS No.: 9036-19-5
Synonyms: Polyoxyethylene octylphenol ether
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2-Aminoheptane (Tuaminoheptane) is a norepinephrine transporter inhibitor. 2-Aminoheptane binds to norepinephrine transporter via ionic and hydrophobic interactions to block norepinephrine uptake. 2-Aminoheptane deactivates ω-TAmla enzyme, reduces recombinant whole cell stability, and acts as an amino group donor substrate for ω-TA and ω-TAmla enzymes. 2-Aminoheptane can be used in research on depression and Alzheimer's disease .
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Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay .
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1 Cited Publications
Cat. No.: HY-10615
CAS No.: 272769-49-0
A-620223 is a PARP-1 inhibitor with a Ki of 8 nM against PARP-1 and EC50 of 3 nM in a whole cell assay. A-620223 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with Temozolomide (TMZ) (HY-17364) and in an MX-1 breast xenograph model in combination with Cisplatin (HY-17394). A-620223 can be used for the studies of melanoma and breast cancer .
Cat. No.: HY-146248B
Purity: 98.02%
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TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research .
Cat. No.: HY-70068
CAS No.: 288150-92-5
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SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor .
Cat. No.: HY-145301
CAS No.: 65840-95-1
Mycobactin-IN-1, a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. Mycobactin-IN-1 inhibits whole-cell drug efflux pumps in M. smegmatis. Mycobactin-IN-1 eradicates intracellularly surviving mycobacteria. Mycobactin-IN-1 shows an excellent in vivo pharmacokinetic profile. Mycobactin-IN-1 can be used for the research of tuberculosis .
Cat. No.: HY-146248
CAS No.: 2412923-11-4
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VU591 is a selective inhibitor of the renal outer medullary potassium channel (ROMK, Kir1.1). VU591 inhibits ROMK via binding to the intracellular pore region near residues Val168 and Asn171, with IC50 of 240 nM in Tl + flux assay and 300 nM in whole cell patch clamp electrophysiology, suppresses native ROMK mediated K + secretion in isolated perfused rat collecting ducts, and exerts antidepressive effects in the mouse tail suspension test (TST). VU591 can be used for the study of ROMK channel function, renal potassium handling, antidepressant mechanisms, and diuretic drug discovery .
Cat. No.: HY-B0753R
CAS No.: 21187-98-4
Synonyms: S1702 (Standard); SE1702 (Standard)
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Gliclazide (Standard) is the analytical standard of Gliclazide. This product is intended for research and analytical applications. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity .
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VU591 hydrochloride is a selective inhibitor of the renal outer medullary potassium channel (ROMK, Kir1.1). VU591 hydrochloride inhibits ROMK via binding to the intracellular pore region near residues Val168 and Asn171, with IC50 of 240 nM in Tl + flux assay and 300 nM in whole cell patch clamp electrophysiology, suppresses native ROMK mediated K + secretion in isolated perfused rat collecting ducts, and exerts antidepressive effects in the mouse tail suspension test (TST). VU591 hydrochloride can be used for the study of ROMK channel function, renal potassium handling, antidepressant mechanisms, and diuretic drug discovery .
Cat. No.: HY-B0753S
CAS No.: 1185039-30-8
Cat. No.: HY-137704
CAS No.: 111864-49-4
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2′-Deoxy-ADPR is an endogenous TRPM2 agonist that activates Ca 2+-permeable cation channels. 2′-Deoxy-ADPR activates the Ca 2+ sensitivity of TRPM2, increasing whole-cell currents by slowing inactivation and increasing open probability. 2′-Deoxy-ADPR can be used in research related to TRPM2 channel-mediated diseases, such as inflammation and immune-related diseases .
Cat. No.: HY-146248A
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TFMU-ADPr triethylamine is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr triethylamine can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr triethylamine binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr triethylamine can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr triethylamine is also applicable to COVID-19-related research .
Cat. No.: HY-125965
CAS No.: 1164475-61-9
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme .
Cat. No.: HY-100841A
CAS No.: 71301-82-1
Synonyms: (S)-3HPG
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(S)-3-Hydroxyphenylglycine ((S)-3HPG) is a metabotropic glutamate receptor (mGluR) agonist with an EC50 of 98 μM in rats. (S)-3-Hydroxyphenylglycine stimulates phosphoinositide hydrolysis, inhibits ACPD-induced depolarization, and exerts weak agonistic and inhibitory effects on mGluR1-mediated signal transduction. (S)-3-Hydroxyphenylglycine selectively activates mGluR1/5, downregulates NMDA receptor channels, reduces NMDA whole-cell currents and intracellular Ca 2+ accumulation, and induces rapid intracellular Ca 2+ oscillations in cortical neurons .
Cat. No.: HY-76612
CAS No.: 1431697-90-3
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SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor .
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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
