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Results for "

threshold

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Calcium Channel (2) Checkpoint Kinase (Chk) (1) Dopamine Receptor (3) Fluorescent Dye (1) GABA Receptor (1) GlyT (1) iGluR (2) mGluR (1) Opioid Receptor (4) Potassium Channel (2) Sigma Receptor (1) Sodium Channel (3) Toll-like Receptor (TLR) (1) TRP Channel (1) Wee1 (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (3) Endocrinology (1) Inflammation/Immunology (5) Neurological Disease (17)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W105835

Magnesium citrate Trimagnesium dicitrate	Toll-like Receptor (TLR)	Neurological Disease
Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active .

HY-D2337

Quinophthalone	Fluorescent Dye	Inflammation/Immunology
Quinophthalone is a dye with distinctive greenish yellow color. Quinophthalone is used as coloring agents for various materials. Quinophthalone is a strong sensitizer in guinea pigs, and its threshold concentration for induction and challenge is 10 ppm .

HY-18961

PD 407824	Checkpoint Kinase (Chk) Wee1	Inflammation/Immunology Cancer
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC₅₀s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .

HY-N2433

Paederosidic acid methyl ester	Potassium Channel	Neurological Disease
Paederosidic acid methyl ester is a ATP‐sensitive K ⁺ channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K ⁺ channel in the brain and spinal cord level .

HY-B1233

Octodrine 2-Amino-6-methylheptane; 1,5-Dimethylhexylamine; 6-Methyl-2-heptylamine	Dopamine Receptor	Others
Octodrine (2-Amino-6-methylheptane) is a central nervous stimulant that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect) .

HY-B1233A

Octodrine hydrochloride 2-Amino-6-methylheptane hydrochloride; 1,5-Dimethylhexylamine hydrochloride; 6-Methyl-2-heptylamine hydrochloride	Dopamine Receptor	Neurological Disease
Octodrine (2-Amino-6-methylheptane) is a central nervous activator that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect) .

HY-121650A

ADTN hydrobromide	Dopamine Receptor	Neurological Disease
ADTN hydrobromide is a long-acting dopamine agonist. ADTN hydrobromide significantly decreases the behavioral visual threshold of DA-IPC-depleted zebrafish .

HY-119061

SB357134	5-HT Receptor	Neurological Disease
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .

HY-100781B

L-AP4 monohydrate L-APB monohydrate	mGluR	Neurological Disease
L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively .

HY-N11975

Glycyrrhizin-6′,6′′-dimethylester	Others	Others
Glycyrrhizin-6′,6′′-dimethylester (compound 23) is a licorice saponin isolated from licorice root. Glycyrrhizin-6′,6′′-dimethylester can participate as an aglycone in the generation of methyl glucuronate, producing similar threshold sweetness, licorice, and bitterness .

HY-19004

711389-S hydrochloride	Others	Cardiovascular Disease
711389-S hydrochloride is an antiarrhythmic compound that demonstrates its antiarrhythmic activity by increasing the ventricular fibrillation threshold (VFT). 711389-S hydrochloride also has strong anti-fibrillation effects and safety, and can be used in the study of ventricular fibrillation and sudden cardiac death .

HY-N7402

Hexyl hexanoate	Others	Others
Hexyl hexanoate is a fruit aroma component with potential food and beverage additive activity. Hexyl hexanoate is found in alcoholic beverages and is used to blend fruit flavors. Hexyl hexanoate is present in many fruits, Parmesan cheese, alcoholic beverages, and black tea. Hexyl hexanoate is a volatile component produced as a result of fruit ripening. Toxicity assessments of hexyl hexanoate showed that it is not mutagenic and that exposure is below safety thresholds for repeated dose, reproduction, and local respiratory toxicity. Hexyl hexanoate is also below thresholds in skin sensitization assessments, and for phototoxicity and photosensitization, the results showed that it does not present a relevant risk. Hexyl hexanoate is considered non-persistent, non-bioaccumulative, and non-toxic according to the environmental criteria of the International Fragrance Association .

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-10635

ABT-102	TRP Channel	Inflammation/Immunology Cancer
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .

HY-111189

GSK931145	GlyT	Neurological Disease
GSK931145 is a glycine transporter 1 (GlyT1) inhibitor with anti-epileptic activity. GSK931145 exhibits a low minimum effective dose in the maximum electrical stimulation threshold test, indicating that it has a significant anti-epileptic effect. GSK931145 is also suitable as a positron emission tomography (PET) radioligand for quantifying the availability of glycine transporters in the living brain .

HY-15292

S107 1 Publications Verification	Calcium Channel Others	Cardiovascular Disease
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca ²⁺ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .

HY-P5869

Kurtoxin	Calcium Channel Sodium Channel	Neurological Disease
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca ²⁺ channel gating inhibitor with a K_d of 15 nM for Cav3.1 (α1G T-type) Ca ²⁺ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca ²⁺ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na ⁺ channel .

HY-P1626

Acetyl tetrapeptide-15	Opioid Receptor	Neurological Disease
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .

HY-P2707

α-Dendrotoxin α-DTX	Sodium Channel Potassium Channel	Others
α-Dendrotoxin (α-DTX) is a small molecule peptide neurotoxin isolated from the venom of the African green mamba snake (Dendroaspis angusticeps). α-Dendrotoxin is also a KV1.1, KV1.2, KV1.6 and ASIC channel blocker. α-Dendrotoxin blocks potassium channels, lowers the threshold of neuronal action potentials, and increases the frequency of action potentials, thereby enhancing neuronal excitability. α-Dendrotoxin can be used in neurotoxicology research .

HY-161784

GABAA receptor modular-3	GABA Receptor	Neurological Disease
GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC₅₀ of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .

HY-111011

CR 665 acetate JNJ 38488502 acetate; FE 200665 acetate	Others	Neurological Disease
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.

HY-125928

AA43279	Sodium Channel	Neurological Disease
AA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC₅₀ of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model .

HY-108998

Bisaramil hydrochloride	Others	Cardiovascular Disease
Bisaramil hydrochloride is an antiarrhythmic compound with activity in inhibiting free radical generation. Bisaramil hydrochloride directly blocks sodium currents and exhibits enhanced sodium channel blocking ability. Bisaramil hydrochloride inhibits isoproterenol-induced slow calcium action potentials in cardiomyocytes. Bisaramil hydrochloride reduces heart rate and prolongs the PR, QRS, and QT intervals in the electrocardiogram, showing blocking effects on sodium and potassium channels. Bisaramil hydrochloride reduces cardiac conduction velocity, increases the threshold current for capture and atrial fibrillation, and prolongs the effective refractory period. Bisaramil hydrochloride reduces ventricular arrhythmias and eliminates mortality caused by ventricular fibrillation in ischemic rat hearts .

HY-14218

Ditolylguanidine 2 Publications Verification 1,3-Di-o-tolylguanidine; DTG	Sigma Receptor	Neurological Disease
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with K_i values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer .

HY-15074

SPD-502 NS-1209	iGluR	Neurological Disease
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC₅₀ = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .

HY-15076

SPD-502 sodium NS-1209 sodium	iGluR	Neurological Disease
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC₅₀ = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .

HY-P1319

Nociceptin(1-7)	Opioid Receptor	Inflammation/Immunology
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .

HY-P1319A

Nociceptin(1-7) TFA	Opioid Receptor	Inflammation/Immunology
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .

HY-B0612B

(S)-Lercanidipine	Others	Neurological Disease
(S)-Lercanidipine is a calcium channel blocker with antihypertensive and neuroprotective activities. (S)-Lercanidipine reduces oxidative stress and protects auditory sensory hair cells from noise-induced damage. (S)-Lercanidipine showed significant protective effects on cell viability in in vitro experiments, especially at low concentrations. (S)-Lercanidipine has been found to effectively reduce the hearing threshold of mice after noise stimulation and protect the survival of outer hair cells. The antioxidant properties of (S)-Lercanidipine are reflected in its increased expression of antioxidant enzyme genes and decreased expression of oxidative enzyme genes. (S)-Lercanidipine administration is effective in reducing noise-induced hearing loss both before and after noise exposure. (S)-Lercanidipine may alleviate noise-induced hearing loss and protect the survival of outer hair cells through its antioxidant mechanism .

Cat. No.	Product Name

HY-L0088V

Life Chemicals 50K Diversity Library	50,240 compounds
Life Chemicals presents a number of exclusive Pre-Plated Diversity Sets composed of 50,240 novel compounds with optimal physicochemical properties selected from Life Chemicals collection of newly synthesized items by dissimilarity search with an average Tanimoto threshold of 82%. These Diverse Screening Sets are ideal starting points for customers looking for a wide range of dissimilarity to screen against a number of targets from different classes or where little information is available on targeted protein structure.

Life Chemicals 50K Diversity Library

50,240 compounds

Life Chemicals presents a number of exclusive Pre-Plated Diversity Sets composed of 50,240 novel compounds with optimal physicochemical properties selected from Life Chemicals collection of newly synthesized items by dissimilarity search with an average Tanimoto threshold of 82%. These Diverse Screening Sets are ideal starting points for customers looking for a wide range of dissimilarity to screen against a number of targets from different classes or where little information is available on targeted protein structure.

HY-L133

Cuproptosis Compound Library	215 compounds
Copper is an important co-factor of all biological enzymes, but if the concentration exceeds the threshold of maintaining the homeostasis mechanism, copper will lead to cytotoxicity. This death mechanism has been named "Cuproptosis". The mechanism of cuproptosis distinct from all other known mechanisms of regulated cell death, including apoptosis, pyroptosis, necroptosis, and ferroptosis. Copper combine with the lipoylated components of the tricarboxylic acid cycle (TCA), leading to lipoylated protein aggregation and subsequent loss of iron-sulfur cluster proteins, ultimately resulting in protein toxicity stress and cell death. Studies have shown that the necessary factors for cuproptosis include the presence of glutathione, mitochondrial metabolism of galactose and pyruvate, and glutamine metabolism. Targeted regulation of cuproptosis is a potential choice to treat cancer, rheumatoid arthritis, and other diseases. For example, up-regulation of LIPT1 may inhibit the occurrence and development of tumors by destroying TCA in mitochondria and then inducing cuproptosis. MCE supplies a unique collection of 215 cuproptosis-related compounds, all of which act on the targets or signaling pathways related to cuproptosis and may have in inhibitory or activated effect on cuproptosis. MCE Cuproptosis Library is a useful tool for drug research related to cancer, rheumatoid arthritis, and other diseases.

Cuproptosis Compound Library

215 compounds

Copper is an important co-factor of all biological enzymes, but if the concentration exceeds the threshold of maintaining the homeostasis mechanism, copper will lead to cytotoxicity. This death mechanism has been named "Cuproptosis".

The mechanism of cuproptosis distinct from all other known mechanisms of regulated cell death, including apoptosis, pyroptosis, necroptosis, and ferroptosis.

Copper combine with the lipoylated components of the tricarboxylic acid cycle (TCA), leading to lipoylated protein aggregation and subsequent loss of iron-sulfur cluster proteins, ultimately resulting in protein toxicity stress and cell death. Studies have shown that the necessary factors for cuproptosis include the presence of glutathione, mitochondrial metabolism of galactose and pyruvate, and glutamine metabolism.

Targeted regulation of cuproptosis is a potential choice to treat cancer, rheumatoid arthritis, and other diseases. For example, up-regulation of LIPT1 may inhibit the occurrence and development of tumors by destroying TCA in mitochondria and then inducing cuproptosis.

MCE supplies a unique collection of 215 cuproptosis-related compounds, all of which act on the targets or signaling pathways related to cuproptosis and may have in inhibitory or activated effect on cuproptosis. MCE Cuproptosis Library is a useful tool for drug research related to cancer, rheumatoid arthritis, and other diseases.

Cat. No.	Product Name	Type