excitation

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Dantrolene sodium (Lapatinib ditosylate monohydrate) salt is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Dantrolene sodium hemiheptahydrate (Sodium dantrolene) is the sodium salt form of dantrolene, a hydantoin derivative, and direct-acting skeletal muscle relaxant.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

CY5-SE Ditriethylamine salt is a reactive dye for the labeling of amino-groups in peptides, proteins, and oligonucleotides. Excitation (nm):649, Emission (nm): 670.

FFN 511 hydrochloride is a fluorescent pseudo-neurotransmitters (FFNs) targeting neuronal vesicular monoamine transporter 2 (VMA T2).FFN 511 hydrochloride inhibits the binding of 5-hydroxytryptamine to VMA T2-containing membranes and can be used for labelling of dopaminergic nerve endings in acute slices of in vivo cortex-striatum. The excitation and emission maxima are 406 and 501 nm, respectively.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

Meclinertant (SR 48692) is a neurotensin receptor-1 (NT1) antagonist that blocks neurotensin-induced excitation and can be used to study neurological disorders.

resorufin galactopyranoside is a fluorescent substrate for β-galactosidase.After cleavage by β-galactosidase, the fluorescent portion of resorufin is released and its fluorescence can be used to quantify β-galactosidase activity. It has an excitation light of 570 and an emission light of 580 nm.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

Ac-DEVD-AFC, a fluorogenic substrate, undergoes cleavage by caspase-3, producing a blue fluorescent compound upon excitation at 400 nm, which can be quantified at an emission maximum of 505 nm.

CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.

Diacylglycerols (DAG) are generated through the hydrolysis of membrane phospholipids and function as lipid second messengers by activating protein kinase C (PKC) and modulating cell growth and apoptosis. Additionally, they act as precursors for DAG kinases in the synthesis of phosphatidic acid, a crucial lipid messenger. The compound 1-NBD-decanoyl-2-decanoyl-sn-glycerol incorporates a nitrobenzoxadiazole (NBD) fluorophore at the ω-end of its terminal decanoyl chain, using the structure of 1,2-didecanoyl-sn-glycerol as a model for diacylglycerol. This molecule is expected to exhibit excitation and emission peaks at roughly 470/541 nm, paralleling those of various NBD-labeled phospholipids. Fluorescently labeled lipids, such as this, are instrumental in exploring their interactions with proteins, their uptake by cells and liposomes, and in developing assays for lipid metabolism research.

BOP-JF549 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor® 549. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 549 nm; emission maximum = 571 nm.

DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination with appropriate two photon pulse laser at 710 nm for ~2 ms.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

Enteropeptidase fluorogenic substrate is a substrate for enteropeptidase that contains a 7-amino-4-trifluoromethylcoumarin (AFC) moiety. Enteropeptidase is a serine protease expressed in the proximal small intestine of higher animals that converts inactive trypsinogen to active trypsin by endoproteolytic cleavage. Enteropeptidase recognizes the highly specific amino acid sequence DDDDK on the fluorogenic substrate and cleaves after the lysine residue, releasing the AFC moiety. Enteropeptidase activity is quantified by fluorescent detection of AFC, which displays excitation/emission spectra of 380/500 nm.

BODIPY-C12 Ceramide (B12Cer) is a fluorescently-tagged form of C12 ceramide, with excitation/emission maxima at 505/540 nm, respectively. It is a fluorescently-labeled sphingolipid and has been utilized for quantifying acid sphingomyelinase activity in the plasma of patients with Niemann-Pick disease.

WUN 73823, also known as N,N'-bis-(acid-PEG3)-Benzothiazole Cy5 is a PEG derivative containing a cyanine dye with excitation/emission maximum 649/667 nm and a free terminal carboxyl acid. Terminal carboxylic acid can react with primary amine groups in the presence of of activators (e.g. EDC, or DCC) to form a stable amide bond. The hydophilic PEG spacer increases solubility in aqueous media. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

FITC-labeled ODN 1585 (sodium) effectively induces IFN and TNFα production and serves to assess CpG ODN cellular uptake and localization via confocal laser-scanning microscopy [excitation 495 nm, emission 520 nm] or flow cytometry.

FITC-labeled ODN TTAGGG (sodium) is an inhibitory oligonucleotide that antagonizes TLR9, AIM2, and cGAS, aiding in assessing CpG ODN cellular uptake and localization through confocal laser-scanning microscopy (excitation at 495 nm, emission at 520 nm) or flow cytometry.

GSHtracer is a ratiometric probe designed for the quantification of glutathione (GSH) concentrations. This probe demonstrates a measurable shift in its excitation-emission profile, specifically from 520/580 nm to 430/510 nm, upon binding with GSH.

Benz-AP, a potent photosensitizer, generates singlet oxygen inversely related to Human carboxylesterase 2 (hCES2) activity, showcasing enhanced photocytotoxicity in cancer cells within low hCES2 environments. Moreover, upon Two-photon excitation (TPE), Benz-AP induces the production of reactive oxygen species (ROS), effectively killing cancer cells and tumor spheroids [1].

Basic Blue 20, a red-emitting DNA stain, exhibits relatively narrow excitation and emission spectra, peaking at 633 nm and 677 nm, respectively. Furthermore, it is characterized by its high resistance to photobleaching [1].

FFN270 hydrochloride, a fluorescent tracer for norepinephrine and vesicular monoamine transporters, features dual resolved absorption/excitation peaks that vary with solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm). It serves as a ratiometric fluorescent pH-sensor, highlighting its utility in monitoring norepinephrine.

7-Azido-4-methylcoumarin (AzMC) is a coumarin fluorescent probe for hydrogen sulfide (H2S).1 AzMC selectively fluoresces in the presence of H2S over a panel of reactive nitrogen, oxygen, and sulfur species. AzMC displays excitation/emission maxima of 340/445 nm, respectively. |1. Chen, B., Li, W., Lv, C., et al. Fluorescent probe for highly selective and sensitive detection of hydrogen sulfide in living cells and cardiac tissues. Analyst 138(3), 946-951 (2013).

4-Methylumbelliferyl caprylate (MUCAP) is a fluorogenic substrate for C8 esterase. MUCAP is cleaved by C8 esterase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nm, increasing as pH decreases.

ThioGlo1 is a thiol-reactive fluorescent probe.1,2,3Upon reaction with a thiol group, a fluorescent adduct is formed that displays excitation/emission maxima of 384/513 nm, respectively.2,3It also reacts with sulfite to form a fluorescent adduct with similar spectral characteristics, and interference from sulfite during thiol determination must be accounted for using secondary methods. ThioGlo1 has been used to monitor the oxidative stability of beer. 1.Yang, J.-R., and Langmuir, M.E.Synthesis and properties of a maleimide fluorescent thiol reagent derived from a naphthopyranoneJ. Heterocycl. Chem.28(5)1177-1180(1991) 2.Hoff, S., Larsen, F.S., Anderson, M.L., et al.Quantification of protein thiols using ThioGlo 1 fluorescent derivatives and HPLC separationAnalyst138(7)2096-2103(2013) 3.Lund, M.N., and Andersen, M.L.Detection of thiol groups in beer and their correlation with oxidative stabilityJ. Am. Soc. Brew. Chem.69(3)163-169(2011)

FITC-labeled ODN 2395 (sodium), a class C oligodeoxynucleotide and TLR9 agonist, facilitates the assessment of CpG ODN cellular uptake and localization via confocal laser-scanning microscopy [excitation 495 nm, emission 520 nm] or flow cytometry.

4-Methylumbelliferyl β-D-N,N'-diacetylchitobioside (4-μU-(GlcNAc)2) is a fluorogenic substrate for chitinases and chitobiosidases. 4-μU-(GlcNAc)2 is cleaved by chitinases and chitobiosidases to release the fluorescent moiety 4-μU. 4-μU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high pH (7.12-10.3), respectively, and an emission maximum ranging from 445 to 455 nm, increasing as pH decreases.

EC-17 (disodium salt), a folate receptor alpha (FRα) targeting contrast agent, exhibits fluorescent properties within the visible light spectrum, characterized by peak excitation and emission wavelengths of 470/520 nm, respectively.

LysoFP-NH2 is the fluorescent form of the lysosomal turn-on fluorescent probe for carbon monoxide (CO) lysoFP-NO2 . LysoFP-NH2 is formed when lysoFP-NO2 reacts with CO. It displays excitation/emission maxima of 440/528 nm, respectively.

Enteropeptidase fluorogenic substrate is a substrate for enteropeptidase that contains a 7-amino-4-trifluoromethylcoumarin (AFC) moiety. Enteropeptidase is a serine protease expressed in the proximal small intestine of higher animals that converts inactive trypsinogen to active trypsin by endoproteolytic cleavage.1,2Enteropeptidase recognizes the highly specific amino acid sequence DDDDK on the fluorogenic substrate and cleaves after the lysine residue, releasing the AFC moiety. Enteropeptidase activity is quantified by fluorescent detection of AFC, which displays excitation/emission spectra of 380/500 nm.3

Suc-YVAD-AMC is a fluorogenic substrate for caspase-1. Upon enzymatic cleavage by caspase-1, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify caspase-1 activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

FAM-DEALAHypYIPMDDDFQLRSF is a 5,6-carboxyfluorescein (FAM) labeled HIF-1α peptide. It binds with high affinity to von Hippel-Lindau (VHL) protein (KD= 3 nM). Can be used to assess ligand binding to VHL in a direct fluorescence polarization (FP) displacement assay. Excitation/emission maxima (λ) = 485/520 nm. This product is a longer peptide version of FAM-DEALA-Hyp-YIPD.

Fendiline is a coronary vasodilator that inhibits calcium function in muscle cells in excitation-contraction coupling; proposed as an antiarrhythmic and antianginal agent.

Optovin is a TRPA1 activator, which is reversibly photoactivated.

7-Acetoxy-1-methylquinolinium iodide (AMQI) serves as a fluorogenic substrate for cholinesterase, with excitation (Ex) at 320 nm and emission (Em) at 410 nm. In a fluorometric flow system, the hydrolysis of AMQI is used to detect and identify inhibitors.

BOP-JF646 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor®646. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 655 nm; emission maximum = 672 nm.

Green fluorescent taxol derivative. Used for microtubule imaging. Binds microtubules with high affinity (Ka ~ 107M-1). Excitation/emission maximum λ ~ 496/526 nm. Lillo et al (2002) Location and properties of the Tax. binding center in microtubules: a picosecond laser study with fluorescent taxoids. Biochemistry. 41 12436 PMID:12369834 |Diaz et al (2000) Molecular recognition of Tax. by microtubules. Kinetics and thermodynamics of binding of fluorescent Tax. derivatives to an exposed site. J.Biol.Chem. 275 26265 PMID:10818101

Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

4-Methylumbelliferyl-α-L-iduronide (free acid) is a fluorogenic substrate for α-L-iduronidase, an enzyme found in cell lysosomes that is involved in the degradation of glycosaminoglycans such as dermatan sulfate and heparin sulfate. 4-Methylumbelliferyl-α-L-iduronide is cleaved by α-L-iduronidase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nM, increasing as pH decreases. This substrate is used in assays that measure the activity of α-L-iduronidase, which is commonly deficient in a type of lysosomal storage disease called mucopolysaccharidosis.

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm

Ac-LETD-AFC is a fluorescent substrate specifically cleaved by caspase-8 and can be used to quantify caspase activity by fluorescence detection of free AFC.Ac-LETD-AFC has an excitation wavelength of 400 nm and an emission wavelength of 505 nm.

Coumarin boronic acid pinacolate ester (CBE) is a more soluble form of coumarin boronic acid that can be used to detect peroxynitrite , hypochlorous acid, and hydrogen peroxide. Peroxynitrite oxidizes CBE into the fluorescent product 7-hydroxycoumarin (COH), which displays excitation/emission maxima of 332/470 nm, respectively.

Z-VAD-AMC is a fluorogenic substrate for caspase-1. Upon enzymatic cleavage by caspase-1, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify caspase-1 activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

CELT-426 is a potent, partially selective fluorescent antagonist of the human D2 dopamine receptor, exhibiting Ki values of 89.3 nM, 194.8 nM, and 263.6 nM for D2, D3, and D4 dopamine receptors, respectively, in radioligand binding assays. This compound serves as an effective fluorescent probe for dopamine receptors, facilitating its application in a range of techniques including fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays. It provides an alternative to GPCR radiolabeling ligands. CELT-426 possesses excitation and emission maxima (λ) of 560 nm and 571 nm, respectively, making it suitable for use as an acceptor dye in Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) assays in conjunction with the CoraFluor1 TR-FRET donor.

CELT-133 is a selective fluorescent antagonist for the hα1A adrenergic receptor, demonstrating complete selectivity towards α1A over α2A receptors, with a Ki of 5 nM and 15% displacement at 1 μM in radioligand binding assays, respectively. It displays equivalent affinity across all α1 adrenergic receptor subtypes. Notably, CELT-133 features excitation and emission maxima (λ) at 560 and 571 nm, respectively, making it suitable for use as an acceptor dye in time-resolved Förster resonance energy transfer (TR-FRET) assays when paired with the CoraFluor 1 TR-FRET donor.

R-BC154 is a high affinity fluorescent α4β1/α9β1 inhibitor (Kdvalues are 12.7 and 38 nM, respectively); fluorescent version of BOP. Rapidly and preferentially mobilizes HSCs and progenitorsin vivo. Excitation maximum, 561 nm; emissiosn maximum, 585 nm.

BODIPY-Palmitate, a fluorescent derivative of palmitic acid, exhibits excitation and emission maxima at 488 nm and 508 nm, respectively. It is employed in the monitoring of fatty acid uptake and metabolism within cultured cells.