Search Result
Results for "
full agonist
" in MedChemExpress (MCE) Product Catalog:
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100369A
-
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GABA Receptor
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Neurological Disease
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DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .
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- HY-155318A
-
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Orphan Receptor
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Endocrinology
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GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM .
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-
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- HY-P1198
-
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
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-
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- HY-145364
-
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GHSR
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Metabolic Disease
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Ghrelin receptor full agonist-2 (compound 12j) is a highly potent Ghrelin receptor full agonist.
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-
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- HY-16619
-
-
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- HY-146733
-
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- HY-128040
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-
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- HY-111359
-
-
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- HY-149941
-
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Neurotensin Receptor
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Neurological Disease
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hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
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-
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- HY-119060
-
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mGluR
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Neurological Disease
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FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively .
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-
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- HY-147511
-
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PPAR
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Others
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PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM) .
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-
-
- HY-W909149
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-
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- HY-120456
-
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Opioid Receptor
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Neurological Disease
|
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SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
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-
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- HY-P1198A
-
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
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- HY-150028
-
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Cannabinoid Receptor
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Inflammation/Immunology
|
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CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
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-
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- HY-146731
-
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PPAR
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Cardiovascular Disease
Metabolic Disease
|
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PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders .
|
-
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- HY-P10377
-
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Neuropeptide FF Receptor
|
Metabolic Disease
|
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GUB03385 is a long-acting PrRP31 analogue. GUB03385 is a potent dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM). GUB03385 has anti-obesity effect .
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-
- HY-148922
-
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PPAR
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Metabolic Disease
|
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PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
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- HY-114116
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-
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- HY-121542
-
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PPAR
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Metabolic Disease
|
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PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .
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-
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- HY-W909173
-
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Trace Amine-associated Receptor (TAAR)
Histamine Receptor
mAChR
|
Neurological Disease
|
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TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC50=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC50=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases .
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-
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- HY-19942A
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-
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- HY-107581
-
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GPR109A
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Metabolic Disease
|
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MK-1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist .
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- HY-114871
-
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GABA Receptor
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Neurological Disease
|
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SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities .
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- HY-101609
-
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E4424
|
5-HT Receptor
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Neurological Disease
|
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Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
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- HY-128855
-
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mAChR
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Neurological Disease
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Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-100856
-
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PTHR
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Endocrinology
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PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
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- HY-N5016
-
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mAChR
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Cardiovascular Disease
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Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors .
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- HY-116490
-
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mAChR
|
Cardiovascular Disease
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Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR .
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-
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- HY-10629
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LXR-623
Maximum Cited Publications
9 Publications Verification
WAY 252623
|
LXR
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Metabolic Disease
Cancer
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LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
|
-
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- HY-13467
-
-
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- HY-P0076
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TAK-448
1 Publications Verification
MVT-602
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Kisspeptin Receptor
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Cancer
|
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TAK-448 (MVT-602) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM .
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- HY-P0076A
-
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MVT-602 acetate
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Kisspeptin Receptor
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Cancer
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TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM .
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-
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- HY-132265
-
-
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- HY-13788
-
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent .
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- HY-13788B
-
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent .
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- HY-N0175
-
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Cytisine; Sophorine; Baptitoxine
|
nAChR
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Metabolic Disease
Cancer
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Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
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- HY-150030
-
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Cannabinoid Receptor
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Neurological Disease
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CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
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- HY-154829A
-
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Neuropeptide FF Receptor
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Inflammation/Immunology
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AC-099 hydrochloride (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 hydrochloride attenuates spinal nerve ligation-induced hypersensitivity in rats .
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- HY-154829
-
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Neuropeptide FF Receptor
|
Inflammation/Immunology
|
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AC-099 (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 attenuates spinal nerve ligation-induced hypersensitivity in rats .
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-
-
- HY-B0659
-
-
-
- HY-169136
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-
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- HY-W329175
-
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SKF-104557
|
Dopamine Receptor
|
Neurological Disease
|
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N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at human D2 and D3 receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor .
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-
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- HY-B0659A
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-
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- HY-121251
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-
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- HY-120223
-
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Adrenergic Receptor
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Metabolic Disease
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BMS-196085 is an orally active, potent and selective full agonist against human β3 adrenergic receptor with a Ki value of 21 nM. BMS-196085 also has partial agonist activity at the β1 receptor. BMS-196085 is promising for research of obesity and type-II diabetes .
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- HY-10019
-
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CP 526555
|
nAChR
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Neurological Disease
Inflammation/Immunology
Cancer
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Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-10020
-
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CP 526555 hydrochloride
|
nAChR
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Neurological Disease
Inflammation/Immunology
Cancer
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Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-10021
-
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CP 526555-18
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nAChR
ERK
p38 MAPK
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Others
Neurological Disease
Cancer
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Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-10019A
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CP 526555 dihydrochloride
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nAChR
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Neurological Disease
Inflammation/Immunology
Cancer
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Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-135432
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APD334 arginine
|
LPL Receptor
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Inflammation/Immunology
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Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
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- HY-137639
-
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HCN Channel
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Neurological Disease
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Sp-8-Br-cGMPS is an analog of cGMP. Sp-8-Br-cGMPS is an agonist for cGMP-gated cation channels (CNG channels), with an EC50 of 106.5 μM. Sp-8-Br-cGMPS induces the currents, without the ability to stabilize the channel open state as a full agonist .
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- HY-B0584
-
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Fluprostenol isopropyl ester; AL6221; Flu-Ipr
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Prostaglandin Receptor
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Cardiovascular Disease
Endocrinology
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Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
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- HY-105634
-
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Progesterone Receptor
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Endocrinology
Cancer
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Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
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- HY-163917
-
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Opioid Receptor
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Neurological Disease
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SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .
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- HY-14340
-
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SAX-187
|
5-HT Receptor
|
Neurological Disease
|
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WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM . WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
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-
- HY-W746031
-
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SAX-187 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
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WAY-181187 (SAX-187) hydrochloride is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM . WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
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- HY-N0175R
-
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nAChR
|
Metabolic Disease
Cancer
|
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Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
|
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- HY-114060
-
-
- HY-162083
-
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Cannabinoid Receptor
5-HT Receptor
|
Neurological Disease
|
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CB2R/5-HT1AR agonist 1 (Compound 2o) is an orally active partial agonist of the CB2 receptor (EC50=479.6 nM). CB2R/5-HT1AR agonist 1 is a full agonist of 5-HT1A receptor (EC50=2.7 μM). CB2R/5-HT1AR agonist 1 exhibits anti-anxiety and anti-depressive effects. CB2R/5-HT1AR agonist 1 possesses favorable pharmacokinetic properties .
|
-
- HY-10680
-
MK-6892
5 Publications Verification
|
GPR109A
|
Cancer
|
|
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
|
-
- HY-P3876
-
-
- HY-139386
-
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15(S)-Flu-Ipr
|
Prostaglandin Receptor
|
Others
|
|
15β-Travoprost (15(S)-Flu-Ipr) is an enantiomer of Travoprost (HY-B0584). Travoprost, an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist .
|
-
- HY-110366
-
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SAX-187 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
-
- HY-B0659S
-
-
- HY-70081
-
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PNU-95666E
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole (PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-10233
-
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Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
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-
- HY-101300
-
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LD 3098 hydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full?α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) .
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-
- HY-10021R
-
|
|
nAChR
ERK
p38 MAPK
|
Others
Neurological Disease
|
|
Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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-
- HY-128344
-
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PARP
Apoptosis
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Metabolic Disease
|
|
BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28 μM and Amax ratio of 98% .
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-
- HY-P3910
-
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Angiotensin Receptor
|
Cardiovascular Disease
|
|
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gαq and βarr2 response, with pEC50 values of 8.31 and 8.44, respectively .
|
-
![[Val4] Angiotensin III](//file.medchemexpress.eu/product_pic/hy-p3910.gif)
- HY-158702
-
|
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5-HT Receptor
|
Neurological Disease
|
|
5-HTQ chloride is an indole alkaloid that can be isolated from the skin secretions of the Australian golden bell frog Litoria aurea. 5-HTQ chloride is also a full agonist of the 5-HT receptor .
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-
- HY-A0007
-
|
N-0923 Hydrochloride
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-15394A
-
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N-0437
|
Adrenergic Receptor
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Endocrinology
|
|
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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-
- HY-108991
-
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(-)-T-0509
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
T-0509 ((-)-T-0509) is a selective full agonist of the β1 receptor. T-0509 activates the cAMP signaling pathway through the β1 receptor and enhances myocardial contractility .
|
-
- HY-P2197
-
-
- HY-108499
-
-
- HY-B0659R
-
|
|
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Brimonidine (Standard) is the analytical standard of Brimonidine. This product is intended for research and analytical applications. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
|
-
- HY-123014
-
|
|
Leukotriene Receptor
|
Cancer
|
|
(Rac)-SC-45694 is a racemate of SC-45694. SC-45694 has full LTB4 agonist activity for neutrophil chemotaxis and has antagonist activity against LTB4-induced neutrophil degranulation .
|
-
- HY-116259
-
|
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PPAR
|
Metabolic Disease
|
|
PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC50 value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro .
|
-
- HY-10019S1
-
|
CP 526555-15N,13C,d2
|
nAChR
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
- HY-10020S
-
|
CP 526555-15N3 Hydrochloride
|
nAChR
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
- HY-160887
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
|
-
- HY-15394
-
|
N-0437 hydrochloride
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-107678
-
|
WAY-317538
|
nAChR
|
Neurological Disease
|
|
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
|
-
- HY-70081A
-
|
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-123942
-
|
|
Toll-like Receptor (TLR)
TNF Receptor
p38 MAPK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
|
-
- HY-A0007R
-
|
N-0923 (Hydrochloride) (Standard)
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-122124
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CAY10583 is a potent and selective full Leukotriene B4 receptor type 2 (BLT2) agonist. CAY10583 directly promotes keratinocyte migration in vitro and accelerates wound closure in vivo. CAY10583 is a promising pharmaceutical agent for diabetic wounds .
|
-
- HY-P2541
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-142972
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .
|
-
- HY-B0584R
-
|
Fluprostenol isopropyl ester(Standard); AL6221(Standard); Flu-Ipr (Standard)
|
Prostaglandin Receptor
|
Endocrinology
|
|
Travoprost (Standard) is the analytical standard of Travoprost. This product is intended for research and analytical applications. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
|
-
- HY-B0659AR
-
|
|
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Brimonidine (tartrate) (Standard) is the analytical standard of Brimonidine (tartrate). This product is intended for research and analytical applications. Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.
|
-
- HY-A0095S
-
|
BIMT-17-d4; BIMT-17BS-d4
|
5-HT Receptor
|
Neurological Disease
|
|
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
|
-
- HY-P2541A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-162689
-
|
|
Free Fatty Acid Receptor
|
Inflammation/Immunology
|
|
GprA is a new synthetic agonist of G-protein-coupled receptor 120/free fatty acid receptor 4 (GPR120/FFAR4), with an AC50 of 203 nM on human GPR120 full isoform. GprA can be used in the research for NAFLD .
|
-
- HY-119222
-
|
|
GPR109A
|
Metabolic Disease
|
|
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia . GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-10019S
-
|
CP 526555-d4
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
|
|
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
|
-
- HY-15394S
-
|
N-0437-d7 hydrochloride
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-10019AS1
-
|
|
Isotope-Labeled Compounds
nAChR
|
Inflammation/Immunology
|
|
Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
|
-
- HY-119222A
-
|
|
GPR109A
|
Metabolic Disease
|
|
GSK256073 tris is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 tris acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia . GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-15394S1
-
|
N-0437-d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
Dopamine Receptor
5-HT Receptor
|
Endocrinology
|
|
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-161671
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice .
|
-
- HY-14782A
-
|
SLV313 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
|
|
Adoprazine (SLV313) hydrochloride is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine hydrochloride is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine has the characteristics of atypical antipsychotics .
|
-
- HY-P1096
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
|
-
- HY-111232
-
|
|
GHSR
|
Metabolic Disease
|
|
GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research .
|
-
- HY-P3057
-
-
![[D-Trp11]-Neurotensin](//file.medchemexpress.eu/product_pic/hy-p3057.gif)
- HY-14782
-
|
SLV313
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics .
|
-
- HY-B0584A
-
|
5,6-trans-Fluprostenol isopropyl ester; 5,6-trans-AL6221; 5,6-trans-Flu-Ipr
|
Prostaglandin Receptor
|
Endocrinology
|
|
5,6-trans-Travoprost is the isomer of Travoprost (HY-B0584), and can be used as an experimental control. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
|
-
- HY-B1532
-
|
(S)-Anabasine; (+)-Anabasine
|
nAChR
|
Neurological Disease
|
|
Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical?pesticide?nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 μM) .
|
-
- HY-W014928
-
|
(S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM) .
|
-
- HY-14147
-
|
BRL 24924
|
5-HT Receptor
|
Metabolic Disease
|
|
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist . Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study .
|
-
- HY-117799
-
|
|
5-HT Receptor
|
Endocrinology
|
|
LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
|
-
- HY-136631
-
|
|
Glucokinase
|
Metabolic Disease
|
|
PF-04279405 is a potent and full-acting glucokinase (GK) agonist (EC50=23 nM). Glucokinase (GK) is an enzyme responsible for the conversion of glucose to glucose-6-phosphate and plays a key role in maintaining blood glucose homeostasis. PF-04279405 can be used in the research of type 2 diabetes .
|
-
- HY-P3584A
-
|
(Pro3) Gastric Inhibitory Peptide, human TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
|
-
- HY-117799A
-
|
|
5-HT Receptor
|
Endocrinology
|
|
LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
|
-
- HY-101299A
-
|
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity . Dihydrexidine can stimulate YAP phosphorylation .
|
-
- HY-101299B
-
|
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity . Dihydrexidine hydrochloride can stimulate YAP phosphorylation .
|
-
- HY-P3584
-
|
(Pro3) Gastric Inhibitory Peptide, human
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes .
|
-
- HY-W654077
-
|
BPAF-d4; 4,4'-(Perfluoropropane-2,2-diyl)diphenol-d4
|
Estrogen Receptor/ERR
|
Endocrinology
|
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
|
-
- HY-W050122
-
|
|
GABA Receptor
|
Neurological Disease
|
|
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
|
-
- HY-10435
-
|
(±)-SKF-82958; Chloro-APB
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
|
-
- HY-134988
-
|
|
FXR
Phosphatase
Cytochrome P450
|
Inflammation/Immunology
|
|
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
|
-
- HY-10435A
-
|
(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
|
-
- HY-B1532R
-
|
|
nAChR
|
Neurological Disease
|
|
Anabasine (Standard) is the analytical standard of Anabasine. This product is intended for research and analytical applications. Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 μM) .
|
-
- HY-119486A
-
|
(Rac)-PF-06649751; (Rac)-CVL-751
|
Dopamine Receptor
Arrestin
|
Neurological Disease
|
|
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
|
-
- HY-135483A
-
|
|
nAChR
|
Neurological Disease
|
|
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
|
-
- HY-135581
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-135582
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-136233
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-136233A
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-P2380
-
|
TFRGAP
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR3 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR3 and residues 39-44 of the full-length human sequence. PAR3 (1-6) activates p42/44 MAPK signaling in fibroblasts expressing PAR1, but not PAR3, an effect that can be blocked by the PAR1 antagonist RWJ 56110.
|
-
- HY-120423
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability . AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-A0095S1
-
|
BIMT-17-d4-1; BIMT-17BS-d4-1
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
|
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
|
-
- HY-106993
-
|
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P2161
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
-
- HY-P2161B
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
-
- HY-106993A
-
|
GT-2331 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-152251
-
|
|
Cannabinoid Receptor
FAAH
|
Inflammation/Immunology
|
|
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production .
|
-
- HY-P2161A
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
-
- HY-111241
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SV 293 is a selective antagonist with neutral antagonist activity. SV 293 binds to human D2 receptors with 100-fold higher affinity and has lower affinity for human D3 and D4 dopamine receptor subtypes. SV 293 was found to block the effects of the full agonist quinpirole in forskolin-dependent adenylate acylase inhibition assays and electrophysiological assays. SV 293 can be used as a useful pharmacological tool to study the role of dopamine D2-like receptor subtypes in dopamine pathways associated with neurological, neuropsychiatric and movement disorders .
|
-
- HY-135581S1
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
|
-
- HY-135582S1
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
|
-
- HY-135582S
-
|
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1198
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
|
-
- HY-P0076
-
TAK-448
1 Publications Verification
MVT-602
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-448 (MVT-602) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM .
|
-
- HY-P0076A
-
|
MVT-602 acetate
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM .
|
-
- HY-P3910
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gαq and βarr2 response, with pEC50 values of 8.31 and 8.44, respectively .
|
-
- HY-P2197
-
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-P1198A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
|
-
- HY-P10377
-
|
|
Neuropeptide FF Receptor
|
Metabolic Disease
|
|
GUB03385 is a long-acting PrRP31 analogue. GUB03385 is a potent dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM). GUB03385 has anti-obesity effect .
|
-
- HY-P3876
-
-
- HY-110366
-
|
SAX-187 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
-
- HY-P2541
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-P2541A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-P1096
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
|
-
- HY-P3057
-
-
- HY-P3584A
-
|
(Pro3) Gastric Inhibitory Peptide, human TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
|
-
- HY-P3584
-
|
(Pro3) Gastric Inhibitory Peptide, human
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes .
|
-
- HY-P2380
-
|
TFRGAP
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR3 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR3 and residues 39-44 of the full-length human sequence. PAR3 (1-6) activates p42/44 MAPK signaling in fibroblasts expressing PAR1, but not PAR3, an effect that can be blocked by the PAR1 antagonist RWJ 56110.
|
-
- HY-P2161
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
-
- HY-P2161B
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
-
- HY-P2161A
-
|
|
Kisspeptin Receptor
|
Cancer
|
|
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-A0095S1
-
|
|
|
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
|
-
-
- HY-B0659S
-
|
|
|
Brimonidine-d4 is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
|
-
-
- HY-10019S1
-
|
|
|
Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-10020S
-
|
|
|
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-A0095S
-
|
|
|
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
|
-
-
- HY-10019S
-
|
|
|
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
|
-
-
- HY-15394S
-
|
|
|
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
-
- HY-10019AS1
-
|
|
|
Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
|
-
-
- HY-15394S1
-
|
|
|
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
-
- HY-W654077
-
|
|
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
|
-
-
- HY-135581S1
-
|
|
|
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
|
-
-
- HY-135582S1
-
|
|
|
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
|
-
-
- HY-135582S
-
|
|
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-128855
-
|
|
|
Alkynes
|
|
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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