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Results for "

thresholds

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Calcium Channel (2) Dopamine Receptor (1) mGluR (1) Opioid Receptor (4) Potassium Channel (1) Sigma Receptor (1) Sodium Channel (1) Toll-like Receptor (TLR) (1) TRP Channel (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (3) Neurological Disease (10)

Inhibitors & Agonists

Screening Libraries

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-18961

PD 407824
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-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-P5799

ω-Conotoxin MVIID SNX-238	Calcium Channel	Neurological Disease
ω-Conotoxin MVIID (SNX-238) is a Conus peptide that blocks an ω-Conotoxin-GVIA-sensitive, high-threshold Ca ²⁺ current in fish retinal ganglion cells .

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-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-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-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-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-15292

S107 1 Publications Verification	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-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-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 .

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	188 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 188 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

188 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 188 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.

ADTN hydrobromide	Biochemical Assay Reagents
ADTN hydrobromide is a long-acting dopamine agonist. ADTN hydrobromide significantly decreases the behavioral visual threshold of DA-IPC-depleted zebrafish .

Cat. No.	Product Name	Target	Research Area