Search Result
Results for "
potentiate
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-134598A
-
|
Epigenetic Reader Domain
|
Cancer
|
653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM .
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-
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- HY-131032
-
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Adenosine Receptor
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Others
|
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively .
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-
-
- HY-14611
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DFB
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mGluR
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Neurological Disease
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3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
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-
-
- HY-164704
-
-
-
- HY-116859
-
-
-
- HY-134598
-
|
Epigenetic Reader Domain
|
Cancer
|
653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM .
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-
-
- HY-103341
-
-
-
- HY-W769935
-
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Others
|
Metabolic Disease
|
5-POHSA, a fatty acid esters of hydroxy fatty acid (FAHFA), potentiates glucose transport .
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-
-
- HY-15276
-
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PARP
|
Cancer
|
4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells .
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-
-
- HY-149157
-
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Others
|
Metabolic Disease
|
L-Lysine orotate is a salt of L-lysine and orotic acid that can potentiate the toxicity of an extract of the mushroom Amanita phalloides .
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-
-
- HY-139628
-
|
Bacterial
|
Infection
Cancer
|
JPD447, a MAC-0547630 derivative, is a novel class of UppS inhibitor to potentiate β-lactam antibiotics.
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-
-
- HY-156009
-
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Others
|
Infection
|
CDFI is an inhibitor of the lipid II flippase MurJ. CDFI potentiates the activity of β-lactams against MRSA .
|
-
-
- HY-101353
-
(-)-LY 235959
|
iGluR
|
Neurological Disease
|
LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics .
|
-
-
- HY-B1429
-
-
-
- HY-124702
-
|
Potassium Channel
|
Cardiovascular Disease
|
ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2 .
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-
-
- HY-101179
-
-
-
- HY-100957
-
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Others
|
Cardiovascular Disease
|
Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides .
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-
-
- HY-160424
-
Diethylamine NONOate sodium; Diethylamine nitric oxide sodium
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Others
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Others
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DEANO sodium is notric oxide donor. DEANO sodium potentiates the abilitv of hypoxanthine/xanthine oxidase to induce lipid peroxidation as well as DNA single- and double-strand breaks .
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-
-
- HY-P3969
-
-
-
- HY-119360
-
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Others
|
Others
|
Lilly 18947 (free base) is a selective drug-potentiating agent that synergizes carbamate insecticides. Lilly 18947 (free base) inhibits a variety of detoxication mechanisms in mammals .
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-
-
- HY-10932
-
Ro 13-5057
|
nAChR
iGluR
|
Neurological Disease
|
Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
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-
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- HY-N1944A
-
|
Bacterial
|
Infection
|
cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics .
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-
-
- HY-119936
-
|
CFTR
Autophagy
|
Inflammation/Immunology
|
GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM .
|
-
-
- HY-101372A
-
|
mAChR
|
Neurological Disease
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
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-
-
- HY-N0857
-
-
-
- HY-100690
-
|
Others
|
Cancer
|
NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer .
|
-
-
- HY-P3578
-
|
Insulin Receptor
|
Endocrinology
|
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
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-
-
- HY-P3985
-
Bradykinin potentiating peptide B
|
Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
Others
|
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
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-
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- HY-124264
-
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iGluR
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Neurological Disease
|
UBP710 is a selective NMDA receptor modulator. UBP710 displays greater activity in potentiating GluN2B-containing receptors than those containing GluN2A .
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-
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- HY-P4685
-
|
Angiotensin Receptor
|
Metabolic Disease
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
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-
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- HY-B0089
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BAY g 5421
|
Glucosidase
|
Metabolic Disease
Cancer
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
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-
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- HY-134220
-
|
Parasite
|
Infection
|
Doramectin monosaccharide is an acid degradation product of Doramectin (HY-17035), a disaccharide-containing anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. Doramectin undergoes acid-catalyzed hydrolysis to form doramectin monosaccharide.
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-
-
- HY-W003576
-
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Cholinesterase (ChE)
Others
|
Neurological Disease
|
ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
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-
-
- HY-116205
-
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Others
|
Others
|
UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
|
-
-
- HY-10932R
-
|
nAChR
iGluR
|
Neurological Disease
|
Aniracetam (Standard) is the analytical standard of Aniracetam. This product is intended for research and analytical applications. Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
-
- HY-B0089A
-
Bay-g 5421 sulfate
|
Glucosidase
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
-
- HY-124867
-
|
TSH Receptor
|
Endocrinology
|
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro .
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-
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- HY-106892
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348U87
|
DNA/RNA Synthesis
|
Infection
|
BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
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-
-
- HY-W415004
-
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Cholinesterase (ChE)
Others
|
Neurological Disease
|
ACHE-IN-38 (Compound mol-8) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
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-
-
- HY-102063
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Pyridoxol, cyclic 3,4-hydrogen phosphate
|
P2X Receptor
|
Neurological Disease
|
MRS 2219 (Pyridoxol) is a selective pharmacological probe of P2X1 receptor. MRS 2219 selectively potentiated ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM .
|
-
-
- HY-15044
-
|
PARP
|
Neurological Disease
Cancer
|
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer agents. NU1025 has anti-cancer and neuroprotective activity .
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-
-
- HY-161870
-
|
Antibiotic
|
Infection
|
Antibiotic adjuvant 1 (compound 3e) is an antibiotic adjuvant that presents insufficient antibacterial activity (MIC > 128 µg/mL) and potentiate the activity of Cloxacillin (HY-B0466A)(66-fold) with synergistic effect .
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-
-
- HY-112209
-
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mAChR
|
Neurological Disease
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
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-
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- HY-120105
-
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DNA/RNA Synthesis
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Cancer
|
NSC666715 is a strand-displacement activity of DNA polymerase inhibitor. NSC666715 potentiates Temozolomide (HY-17364)-induced DNA damage, cell senescence and apoptosis. NSC666715 can be used for study colorectal cancer .
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-
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- HY-N7038
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PHA-M
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Others
|
Inflammation/Immunology
|
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis .
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-
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- HY-135572
-
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Others
|
Neurological Disease
Cancer
|
TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity .
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-
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- HY-P4012
-
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Vasopressin Receptor
|
Endocrinology
|
[Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture .
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-
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- HY-14612
-
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mGluR
|
Neurological Disease
|
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
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-
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- HY-N3995
-
|
Apoptosis
Drug Metabolite
|
Cancer
|
5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
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-
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- HY-117517
-
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Others
|
Cancer
|
NG-012, potentiator of nerve growth factor (NGF), were isolated from the culture broth of Penicillium verruculosum F-4542. NG-012 potentiates the neurite outgrowth induced by NGF in rat pheochromocytoma cell line (PC12) .
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-
- HY-106611
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SR 33287
|
Phospholipase
|
Cancer
|
Brinazarone (SR 33287) is an inhibitor for acid lysosomal sphingomyelinase, and leads to cellular lipidosis. Brinazarone potentiates the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells .
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- HY-139803
-
|
Neprilysin
Prolyl Endopeptidase (PREP)
|
Cardiovascular Disease
|
SCH-39370 is a potent and specific inhibitor of neutral metalloendopeptidase (NEP) from rabbit kidney with an IC50 value of 11.2 nM. SCH-39370 potentiates biological responses to atrial natriuretic factor and lowers blood pressure in desoxycorticosterone acetate-sodium hypertensive rats .
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- HY-15066
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FG9065
|
iGluR
|
Neurological Disease
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
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-
- HY-112658
-
|
Adrenergic Receptor
Adenosine Receptor
|
Endocrinology
|
p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
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-
- HY-161413
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
Antibacterial agent 204 (Compd P2-56-3) possesses potentiated Rifampin (RIF) activity against Acinetobacter baumannii and Klebsiella pneumoniae. Antibacterial agent 204 (Compd P2-56-3) disrupts the outer membrane of A. baumannii. T .
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-
- HY-N1944AR
-
|
Bacterial
|
Infection
|
cis-Nerolidol (Standard) is the analytical standard of cis-Nerolidol. This product is intended for research and analytical applications. cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics .
|
-
- HY-119993
-
BMH-23
|
DNA/RNA Synthesis
|
Cancer
|
AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .
|
-
- HY-149810
-
|
Bacterial
Parasite
|
Infection
|
AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-106822
-
AO-33; (±)-Losigamone; LSG
|
Sodium Channel
Chloride Channel
|
Neurological Disease
|
Losigamone (AO-33) is an orally active antiepileptic compound. Losigamone blocks sodium channel. Losigamone stimulates the neuronal chloride channel and enhance chloride influx. Losigamone potentiates GABA-mediated responses and reduces epileptiform activity induced by chloride channel antagonists. Losigamone can be used for epilepsy research .
|
-
- HY-114611
-
|
IRE1
|
Metabolic Disease
|
BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
|
-
- HY-100702
-
|
Akt
Apoptosis
|
Cancer
|
SH-5 is a potent AKT inhibitor. SH-5 potentiates the apoptosis induced by tumor necrosis factor. SH-5 blocks NF-kB activation induced by TNF-a, lipopolysaccharide (HY-D1056), phorbol ester (HY-18739), and cigarette smoke .
|
-
- HY-113654
-
|
TRP Channel
|
Others
|
AMG 7905 is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 potentiates TRPV1 channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin .
|
-
- HY-15066A
-
FG9065 disodium
|
iGluR
|
Neurological Disease
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
|
-
- HY-149811
-
|
Bacterial
Parasite
|
Infection
|
Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-149812
-
|
Bacterial
Parasite
|
Infection
|
Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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-
- HY-B1811
-
|
Endogenous Metabolite
|
Neurological Disease
|
Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
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-
- HY-119226
-
|
mAChR
|
Neurological Disease
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
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-
- HY-12390
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Lopramine
|
Others
|
Neurological Disease
|
Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties .
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-
- HY-N125722
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Aabomycin A1
|
ATP Synthase
Antibiotic
|
Infection
|
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
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-
- HY-14658
-
Thalidomide
Maximum Cited Publications
15 Publications Verification
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
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-
- HY-12390A
-
Lopramine hydrochloride
|
Others
|
Neurological Disease
|
Lofepramine (Lopramine) hydrochloride is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine hydrochloride stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine hydrochloride may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine hydrochloride has significant anxiolytic efficacy in addition to its antidepressant properties .
|
-
- HY-162472
-
|
ATM/ATR
DNA-PK
|
Cancer
|
XRD-0394 is a potent and specific dual inhibitor of ATM and DNA-PKcs with oral activity. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. In addition, XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
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- HY-120547
-
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Others
|
Neurological Disease
Metabolic Disease
|
UCB-11056 is a modulator of cyclic AMP generation. UCB-11056 can rapidly increase cyclic AMP levels in the rat brain in vivo and potentiate stimulated cyclic AMP formation in vitro. UCB-11056 does not stimulate cAMP formation on its own. UCB-11056 is a potential nootropic drug .
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-
- HY-W654264
-
|
Endogenous Metabolite
Integrin
|
Cardiovascular Disease
|
2-Methylbutyrylcarnitine (chloride) is a gut microbial metabolite which binds to integrin α2β1 in platelets, potentiating cytosolic phospholipase A2 (cPLA2) activation and platelet hyperresponsiveness. 2-Methylbutyrylcarnitine (chloride) enhances platelet hyperreactivity and thrombus formation in mice. 2-Methylbutyrylcarnitine (chloride) is a branched-chain acylcarnitine .
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-
- HY-115895
-
CI-686 free base
|
Others
|
Neurological Disease
|
Trebenzomine (CI-686 free base) is a centrally acting psychotropic compound. Trebenzomine has both neuroleptic and stimulant activity. Trebenzomine potentiates Methamphetamine-induced self-stimulation. Trebenzomine reduces septal
hyperirritability, suppression of conditioned avoidance behavior, blocks Apomorphine (HY-12723)-induced emesis in dogs .
|
-
- HY-15519
-
|
IAP
FLT3
|
Cancer
|
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells .
|
-
- HY-120139
-
KMH-233
1 Publications Verification
|
Others
|
Cancer
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-136731
-
|
DNA/RNA Synthesis
|
Cancer
|
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
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-
- HY-153542
-
|
Others
|
Others
|
AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition .
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-
- HY-P5172
-
|
Sodium Channel
|
Neurological Disease
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
|
-
- HY-130656
-
cis-8-Eicosenoic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
8(Z)-Eicosenoic acid is a cis-unsaturated free fatty acid with a 20-carbon chain. It potentiates acetylcholine (ACh) receptor channel currents without depression and enhances PCKε phosphorylation of a substrate peptide in Xenopus oocytes. 8(Z)-Eicosenoic acid constitutes 6% of the fatty acid pool in seed oil isolated from B. collina.
|
-
- HY-142723
-
|
Potassium Channel
|
Neurological Disease
|
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype .
|
-
- HY-103367
-
|
Checkpoint Kinase (Chk)
|
Cancer
|
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
|
-
- HY-P5780
-
|
Sodium Channel
|
Neurological Disease
|
π-TRTX-Hm3a is a 37-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. π-TRTX-Hm3a pH-dependently inhibits acid-sensing ion channel 1a (ASIC1a) with an IC50 of 1-2 nM and potentiates ASIC1b with an EC50 of 46.5 nM .
|
-
- HY-157838
-
|
MAP4K
|
Cancer
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
|
-
- HY-G0021
-
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-B1546A
-
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM .
|
-
- HY-N6733
-
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
Orthopoxvirus
|
Infection
Inflammation/Immunology
|
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line .
|
-
- HY-B1546
-
Benzylamiloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM .
|
-
- HY-N3995S
-
|
Apoptosis
Drug Metabolite
|
Cancer
|
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis[1][2][3][4][5].
|
-
- HY-143498
-
|
DNA/RNA Synthesis
|
Cancer
|
ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells .
|
-
- HY-147349
-
|
Beta-lactamase
Bacterial
|
Infection
|
ANT3310 sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection .
|
-
- HY-101377A
-
(R)-8-Hydroxy-2-dipropylaminotetralin hydrobromide
|
5-HT Receptor
|
Neurological Disease
|
R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent 5-HT1A agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC) .
|
-
- HY-120523
-
|
iGluR
|
Neurological Disease
|
UBP646 is a potent GluN1/GluN2D receptors potentiator, and also potentiates the other three subtypes, GluN1/GluN2A, GluN1/GluN2B, and GluN1/GluN2C receptors .
|
-
- HY-B1811S1
-
|
Isotope-Labeled Compounds
|
Others
|
Vasopressin-d5 is anIsotope-labeled compound of Vasopressin. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-111655
-
SKA-31
3 Publications Verification
|
Potassium Channel
|
Cardiovascular Disease
|
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure .
|
-
- HY-107613
-
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-120645
-
|
Opioid Receptor
|
Neurological Disease
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
|
-
- HY-143415
-
|
Beta-lactamase
Bacterial
|
Infection
|
Metallo-β-lactamase-IN-7 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.019 μM, 13.64 μM, 0.38 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-7 potentiate antibacterial activity of Meropenem against the Gram-negative bacterial strains .
|
-
- HY-107613A
-
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Infection
Inflammation/Immunology
Cancer
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-161681
-
|
Guanylate Cyclase
|
Metabolic Disease
|
Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
|
-
- HY-167825
-
-
- HY-14658R
-
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
|
-
- HY-A0009
-
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-W014622
-
|
DNA/RNA Synthesis
|
Cancer
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
|
-
- HY-122255
-
|
mGluR
|
Neurological Disease
|
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
|
-
- HY-U00244A
-
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
|
Cancer
|
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
|
-
- HY-108985
-
EGYT-3615
|
Others
|
Neurological Disease
|
Trazium esilate (EGYT-3615) is an antidepressant, which influences the central dopaminergic system. Trazium esilate synergizes amphetamine, potentiates stereotypy and hypermotility. Trazium esilate blocks Apomorphine (HY-12723)-induced hypothermic and the stereotypy, and Bulbocapnine (HY-W436270)-induced cataleptic state. Trazium esilate enhances the effect of Norepinephrine (HY-13715) on isolated vas deferens of the rat .
|
-
- HY-100403
-
|
mGluR
|
Cancer
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist?and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
|
-
- HY-12390S
-
|
Isotope-Labeled Compounds
|
Neurological Disease
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
|
-
- HY-B1671
-
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
|
-
- HY-N7426
-
3-Deoxy-D-glucosone
|
GLP Receptor
|
Metabolic Disease
|
3-Deoxyglucosone (3-Deoxy-D-glucosone) is a reactive intermediate of the Maillard reaction and the polyol pathway. 3-Deoxyglucosone rapidly reacts with protein amino groups to form advanced glycation end products (AGEs), such as imidazolone, it is the most specific AGE for 3-DG. 3-Deoxyglucosone synergizes with low glucose to potentiate GLP-1 secretion and is considered as a biomarker for diabetes .
|
-
- HY-124056
-
|
CXCR
|
Cancer
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-16969
-
Dihexa
5 Publications Verification
PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2
|
c-Met/HGFR
|
Neurological Disease
|
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
|
-
- HY-158380
-
|
Bacterial
|
Infection
|
UH-NIP-16 exhibits antimicrobial activity against Mycobacterium tuberculosis, with MIC50 of 1.86 and 3.05 μM, for pathogenic mycobacterial strains H37Rv and CDC1551. UH-NIP-16 synergizes with Streptomycin (HY-B1906), Isoniazid (HY-B0329), Ethambutol (HY-B0535) and Bedaquiline (HY-14881), potentiates their anti-tuberculosis activities .
|
-
- HY-123489
-
THDOC
|
GABA Receptor
|
Neurological Disease
|
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
- HY-103520
-
|
GABA Receptor
|
Neurological Disease
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
|
-
- HY-118140
-
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
|
-
- HY-12976
-
|
G Protein-coupled Receptor Kinase (GRK)
|
Metabolic Disease
|
DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes .
|
-
- HY-12757
-
|
BCRP
|
Cancer
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-103645
-
|
Bacterial
Aurora Kinase
Apoptosis
|
Infection
Cancer
|
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
|
-
- HY-103552
-
|
mGluR
|
Neurological Disease
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
|
-
- HY-G0021S
-
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
|
-
- HY-120553
-
|
Apoptosis
|
Neurological Disease
|
B355252, a phenoxy thiophene sulfonamide small molecule, is a potent NGF receptor agonist. B355252 potentiates NGF-induced neurite outgrowth. B355252 protects ischemic neurons from neuronal loss by attenuating DNA damage, reducing ROS production and the LDH level, and preventing neuronal apoptosis. B355252 has anti-apoptotic effects in glutamate-induced excitotoxicity, as well as in a murine hippocampal cell line (HT22) model of Parkinson disease (PD) .
|
-
- HY-14292
-
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes .
|
-
- HY-150090
-
|
CFTR
|
Inflammation/Immunology
|
SRI-41315 induces a prolonged pause at stop codons and suppresses PTCs (premature termination codons) associated with cystic fibrosis in immortalized and primary human bronchial epithelial cells, restoring CFTR (cystic fibrosis transmembrane conductance regulator) expression and function. SRI-41315 suppresses PTCs by reducing the abundance of the termination factor eRF1. SRI-41315 also potentiates aminoglycoside-mediated readthrough, leading to synergistic increases in CFTR activity .
|
-
- HY-G0021S1
-
Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
|
-
- HY-120139A
-
|
Others
|
Cancer
|
(R)-KMH-233 is the isomer of KMH-233 (HY-120139), and can be used as an experimental control. KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-N8280
-
|
Fungal
|
Infection
|
IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties. It is cytotoxic to L5178Y murine leukemia cells (IC50=0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC=6.25 μg/mL) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.
|
-
- HY-N6733R
-
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
Orthopoxvirus
|
Infection
Inflammation/Immunology
|
Aphidicolin (Standard) is the analytical standard of Aphidicolin. This product is intended for research and analytical applications. Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line .
|
-
- HY-125047
-
UK 3557
|
Monoamine Oxidase
|
Neurological Disease
|
Daledalin tosylate (UK 3557) has mono-amine oxidase inhibitory activity in vitro, probably by acting as a substrate. Daledalin tosylate also has antidepressant effects. Daledalin tosylate potentiates amphetamine-induced excitation in rats, antagonises Reserpine (HY-N0480)-hypothermia in mice, tetrabenazine-sedation in rats and Reserpine (HY-N0480)- and Tetrabenazine (HY-B0590)-induced ptosis in mice with . Daledalin tosylate is proming for rasearch of depressive illness .
|
-
- HY-107506
-
|
mGluR
|
Neurological Disease
|
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
|
-
- HY-A0009S
-
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
|
-
- HY-125604
-
|
Beta-lactamase
Bacterial
|
Infection
|
WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases .
|
-
- HY-117836
-
|
FAK
|
Cancer
|
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
|
-
- HY-A0009R
-
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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- HY-B1671R
-
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GABA Receptor
Sodium Channel
Calcium Channel
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Neurological Disease
Metabolic Disease
|
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
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- HY-B0996
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NSC-17764
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
Hexetidine (NSC-17764) is an orally active antibacterial and antifungal agent with broad antibacterial and antifungal activity. Hexetidine combined with IPBC potentiates strong fungal growth inhibition properties. Hexetidine at concentrations greater than 0.1% can cause oral ulceration. Additionally, Hexetidine improves its plaque inhibiting activities combined with zinc and has been confirmed the effectiveness on purulent wound along with ultrasound. Hexetidine is a promising candidate for research in fungus-related diseases and soft tissue purulent-inflammatory
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- HY-P1210
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Melanocortin Receptor
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Endocrinology
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Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
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- HY-B1803A
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ICI 136753 hydrochloride
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GABA Receptor
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Neurological Disease
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .
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- HY-P1210A
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Melanocortin Receptor
|
Endocrinology
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Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
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- HY-B1692
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MSX; MSO
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Glutaminase
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Neurological Disease
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L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS) .
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- HY-B1811AS1
-
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Isotope-Labeled Compounds
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Neurological Disease
|
Vasopressin-d5 TFA is the TFA salt form of Vasopressin-d5 (HY-B1811S1). Vasopressin-d5 TFA is an isotope-labeled compound of Vasopressin (HY-B1811). Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
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- HY-120184
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AZ13713945
|
mAChR
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Neurological Disease
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VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
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- HY-W016412
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- HY-P2196A
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Apelin Receptor (APJ)
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Cancer
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ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
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-
- HY-123489S
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THDOC-d3
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GABA Receptor
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Neurological Disease
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3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
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- HY-123597
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DDUG; NCI C04808
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Others
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Cancer
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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-
- HY-130349
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L-656,748
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Others
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Infection
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Emamectin B1a is a semisynthetic derivative of avermectin B1a. It binds to GABAA receptors (Ki=17.6 nM in rat brain membranes), including those containing β1, β2, or β3 subunits (IC50s=57, 210, and 49.8 nM for α1β1γ2, α1β2γ2, and α1β3γ2 subunits, respectively), and potentiates the GABA response.2 Emamectin B1a also binds to and inhibits glycine receptors (IC50=218 nM in rat spinal cord). Emamectin B1a induces mortality in 90% of S. exigua larvae in a diet incorporation assay at a dose of 1.067 ng/ml, which is approximately 1,500-fold more toxic than avermectin B1. It is effective against neonate S. eridania larvae in a foliage spray bioassay and when applied topically.
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-
Cat. No. |
Product Name |
Type |
-
- HY-W016412
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CoQ0
|
Enzyme Substrates
|
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3985
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Bradykinin potentiating peptide B
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
Others
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Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
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- HY-P4685
-
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Angiotensin Receptor
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Metabolic Disease
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
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-
- HY-B1811
-
|
Endogenous Metabolite
|
Neurological Disease
|
Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
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-
- HY-P3969
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-
- HY-P3578
-
|
Insulin Receptor
|
Endocrinology
|
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
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-
- HY-P4012
-
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Vasopressin Receptor
|
Endocrinology
|
[Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture .
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-
- HY-P1257
-
|
Peptides
|
Metabolic Disease
|
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
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-
- HY-P1257A
-
|
Peptides
|
Metabolic Disease
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
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-
- HY-P5172
-
|
Sodium Channel
|
Neurological Disease
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
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-
- HY-P5780
-
|
Sodium Channel
|
Neurological Disease
|
π-TRTX-Hm3a is a 37-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. π-TRTX-Hm3a pH-dependently inhibits acid-sensing ion channel 1a (ASIC1a) with an IC50 of 1-2 nM and potentiates ASIC1b with an EC50 of 46.5 nM .
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-
- HY-P1210
-
|
Melanocortin Receptor
|
Endocrinology
|
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-P1210A
-
|
Melanocortin Receptor
|
Endocrinology
|
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-P2196A
-
|
Apelin Receptor (APJ)
|
Cancer
|
ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1944A
-
-
-
- HY-N0857
-
-
-
- HY-B0089
-
-
-
- HY-N7038
-
-
-
- HY-N3995
-
-
-
- HY-B1811
-
-
-
- HY-N125722
-
-
-
- HY-B0089A
-
-
-
- HY-117517
-
-
-
- HY-N1944AR
-
-
-
- HY-W654264
-
-
-
- HY-N6733
-
-
-
- HY-167825
-
-
-
- HY-A0009
-
Galantamine hydrobromide
|
Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
|
Cholinesterase (ChE)
nAChR
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
-
- HY-B1671
-
-
-
- HY-N7426
-
-
-
- HY-N6733R
-
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
Orthopoxvirus
|
Aphidicolin (Standard) is the analytical standard of Aphidicolin. This product is intended for research and analytical applications. Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line .
|
-
-
- HY-A0009R
-
Galantamine hydrobromide (Standard)
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Amaryllidaceae
|
nAChR
Cholinesterase (ChE)
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
-
- HY-B1671R
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-G0021S1
-
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
|
-
-
- HY-B1811AS1
-
|
Vasopressin-d5 TFA is the TFA salt form of Vasopressin-d5 (HY-B1811S1). Vasopressin-d5 TFA is an isotope-labeled compound of Vasopressin (HY-B1811). Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
-
- HY-N3995S
-
|
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis[1][2][3][4][5].
|
-
-
- HY-B1811S1
-
|
Vasopressin-d5 is anIsotope-labeled compound of Vasopressin. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
-
- HY-12390S
-
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
|
-
-
- HY-G0021S
-
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
|
-
-
- HY-A0009S
-
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
|
-
-
- HY-123489S
-
|
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-116629
-
|
|
Alkynes
|
Dactylyne is an ethyl dibromochloroether isolated from the sea hare Dactylomela. Dactylyne has the ability to inhibit Pentobarbital (PTB) metabolism and potentiate the effects of other hypnotic drugs .
|
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