Search Result
Results for "
full agonist
" in MedChemExpress (MCE) Product Catalog:
20
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-10629
-
|
WAY 252623
|
LXR
|
Metabolic Disease
Cancer
|
|
LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
|
-
-
- HY-10019
-
|
CP 526555
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
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 α7β2 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-N0175
-
|
Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
Cancer
|
|
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 .
|
-
-
- HY-10021
-
|
CP 526555-18
|
nAChR
ERK
p38 MAPK
|
Others
Neurological Disease
Cancer
|
|
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-100856
-
|
|
PTHR
|
Endocrinology
|
|
PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
|
-
-
- HY-132265
-
-
-
- HY-121251
-
-
-
- HY-147105
-
|
|
Orphan Nuclear Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
LRH-1 agonist-2 (Compound 6N) is a selective, full LRH-1 agonist with an EC50 of 15.7 nM. LRH-1 agonist-2 directly interacts with the Thr352 and His390 residues in the LRH-1 binding pocket, promotes allosteric signaling to the activation function surface (AFS), stabilizes the AFS and enhances coactivator recruitment. LRH-1 agonist-2 induces the anti-inflammatory cytokine IL-10, and reduces the pro-inflammatory cytokines IL-1β and TNFα. LRH-1 modulator-1 exerts anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 can be used in studies related to inflammatory bowel disease .
|
-
-
- HY-10680
-
|
|
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-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-10233
-
|
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 .
|
-
-
- HY-B0659
-
-
-
- HY-B0659A
-
-
-
- HY-114116
-
-
-
- HY-13788
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-B0584
-
|
Fluprostenol isopropyl ester; AL6221; Flu-Ipr
|
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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-10020
-
|
CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
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-14340
-
|
SAX-187
|
5-HT Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-101300
-
|
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) .
|
-
-
- HY-100369A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-N5016
-
|
|
mAChR
|
Cardiovascular Disease
|
Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors .
|
-
-
- 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-P0076
-
TAK-448
3 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-16619
-
-
-
- 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-114871
-
|
|
GABA Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-10019A
-
|
CP 526555 dihydrochloride
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
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 α7β2 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-P2197
-
-
-
- HY-155318A
-
|
|
Orphan GPCR
|
Endocrinology
|
|
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM .
|
-
-
- HY-116490
-
|
|
mAChR
|
Cardiovascular Disease
|
Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR .
|
-
-
- HY-128855
-
|
|
mAChR
|
Neurological Disease
|
|
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.
|
-
-
- HY-114060
-
-
-
- HY-N0175R
-
|
Cytisine (Standard); Sophorine (Standard); Baptitoxine (Standard)
|
Reference Standards
nAChR
|
Metabolic Disease
Cancer
|
|
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 .
|
-
-
- 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-108499
-
-
-
- HY-145364
-
|
|
GHSR
|
Metabolic Disease
|
|
Ghrelin receptor full agonist-2 (compound 12j) is a highly potent Ghrelin receptor full agonist.
|
-
-
- HY-108991
-
|
(-)-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-19942A
-
-
-
- HY-135432
-
|
APD334 arginine
|
LPL Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-B0659S
-
-
-
- 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-128040
-
-
-
- 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-101609
-
|
E4424
|
5-HT Receptor
|
Neurological Disease
|
|
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
|
-
-
- HY-175490
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγ inverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC50 values of 0.4 and 0.9 μM for Gal4-RORγ and full-length RORγ, respectively. RORγ inverse agonist 2 is useful in the study of autoimmune diseases .
|
-
-
- HY-P5131
-
|
|
Opioid Receptor
|
Others
|
|
[Dmt1]DALDA is a potent and long-acting analgesic binds to the mu opioid receptor with high affinity and selectivity. [Dmt1]DALDA is a full agonist at hMOR (Kd = 0.199 nM) and hDOR, but only partial agonist against hKOR .
|
-
-
- HY-154829A
-
|
|
Neuropeptide FF Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-105634
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
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.
|
-
-
- HY-W746031
-
|
SAX-187 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-P3876
-
-
- HY-70081
-
|
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-10021R
-
|
CP 526555-18 (Standard)
|
Reference Standards
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 .
|
-
- HY-100369AR
-
|
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
|
DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. 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 .
|
-
- HY-146733
-
-
- HY-180210
-
|
|
GHSR
GHR
IGF-1R
|
Inflammation/Immunology
Cancer
|
|
Ghrelin receptor full agonist-3 (Compound 22) is a selective, potent and orally active ghrelin receptor full agonist with an EC50 of 1.8 nM. Ghrelin receptor full agonist-3 can stimulate pulsatile secretion of growth hormone (GH), significantly increasing the frequency and duration of GH secretion, thereby inducing a sustained increase in insulin-like growth factor-1 (IGF-1) levels. Ghrelin receptor full agonist-3 can be used for the researches of cancer and chronic obstructive pulmonary disease .
|
-
- HY-111359
-
-
- 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-119060
-
|
|
mGluR
|
Neurological Disease
|
|
FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively .
|
-
- 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-147511
-
|
|
PPAR
|
Others
|
|
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) .
|
-
- HY-120456
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-W909149
-
-
- HY-146731
-
|
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
|
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 .
|
-
- HY-150028
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-148922
-
|
|
PPAR
|
Metabolic Disease
|
|
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 .
|
-
- HY-121542
-
|
|
PPAR
|
Metabolic Disease
|
|
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 .
|
-
- HY-W909173
-
|
|
Trace Amine-associated Receptor (TAAR)
Histamine Receptor
mAChR
|
Neurological Disease
|
|
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 .
|
-
- HY-19942
-
-
- HY-13788B
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-154829
-
|
|
Neuropeptide FF Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-150030
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-169136
-
-
- HY-120915
-
|
|
mAChR
|
Neurological Disease
|
|
L 689660 maleate, a cholinomimetic agent, is a selective M1 and M3 muscarinic receptors agonist. L 689660 maleate is a potent M1 muscarinic receptor full agonist in the rat superior cervical ganglion (pEC50 of 7.3). L 689660 maleate is a potent M3 receptors agonist in the guinea-pig ileum myenteric plexus-longitudinal muscle or in trachea (pEC50 of 7.5 and 7.7, respectively) .
|
-
- HY-W664041
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Noncatechol agonist-1 (19) is a Noncatechol agonist with full efficacy at both D1R-G protein and D1R-β-arrestin2 pathways, with pEC50 values of 8.41 for D1R-mediated cAMP production and 7.7 for β-arrestin2 recruitment, respectively .
|
-
- HY-W329175
-
|
SKF-104557
|
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-19294
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BMS-201620 is a selective β3 full agonist, with a Ki of 93 nM. BMS-201620 can be used in the research of obesity and non-insulin-dependent diabetes .
|
-
- HY-120223
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-163917
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-137639
-
|
|
HCN Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-139386
-
|
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-W743727
-
|
|
Isotope-Labeled Compounds
nAChR
|
Metabolic Disease
|
|
Cytisine-d4 is the deuterium labeled Cytisinicline (HY-N0175). 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 .
|
-
- 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-162083
-
|
|
Cannabinoid Receptor
5-HT Receptor
|
Neurological Disease
|
|
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-128344
-
|
|
PARP
Apoptosis
|
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% .
|
-
- HY-158702
-
|
|
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 .
|
-
- HY-10019R
-
|
CP 526555 (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline (Standard) is the analytical standard of Varenicline. 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 α7β2 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-10019AR
-
|
CP 526555 dihydrochloride (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. 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 α7β2 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-10020R
-
|
CP 526555 hydrochloride (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline (Hydrochloride) (Standard) is the analytical standard of Varenicline (Hydrochloride). 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 .
|
-
- HY-15394A
-
|
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.
|
-
- 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-B0659R
-
|
UK 14304 (Standard); AGN190342 (Standard)
|
Reference Standards
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-116259
-
|
|
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-186122
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC50 of 48 nM against wild-type CCK-2R and an IC50 of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain .
|
-
- HY-180465
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
5-HT2C agonist-12 (example.2) is a selective and orally active 5-HT2C receptor agonist. 5-HT2C agonist-12 can inhibit the accumulation of IP3 with an IC50 of 4.5 nM. 5-HT2C agonist-12 can induce a feeling of fullness, shorten the time of eating, and reduce calorie intake. 5-HT2C agonist-12 can be used for the research of obesity .
|
-
- HY-P11810
-
|
|
GnRH Receptor
Neuropeptide FF Receptor
|
Metabolic Disease
|
|
GUB08248 is a full GPR10 agonist and a partial NPFF2R agonist, with EC50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 inhibits food intake and induces sustained weight loss. GUB08248 can be used in obesity-related research .
|
-
- HY-P11432
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
PG-911 is a full MC5R agonist (EC50 = 0.031 nM for hMC5R). PG-911 is also a full antagonist at the hMC3R and the hMC4R (Kb: 0.38 nM and 0.17 nM, respectively). PG-911 can be used in the research of neurological disorders .
|
-
- HY-13467A
-
-
- HY-W414109
-
|
|
Opioid Receptor
Arrestin
|
Neurological Disease
|
|
ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia .
|
-
- HY-182551
-
|
|
Neurotensin Receptor
|
Others
Neurological Disease
|
|
SR-12062 is a Neurotensin receptor 1 (NTSR1) full agonist that modulates NTSR1 to trigger intracellular Ca 2+ mobilization. SR-12062 can be used for the research of schizophrenia, parkinson’s disease, drug addiction .
|
-
- HY-18176
-
|
|
nAChR
Potassium Channel
|
Neurological Disease
|
|
SEN 78702 is an orally active, selective, full α7 nAChR agonist, with a pEC50 of 6.13. SEN 78702 has an acceptable hERG inhibition (IC50: 15.8 μM). SEN 78702 induces memory enhancement .
|
-
- HY-10019S2
-
|
CP 526555-13C,15N
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. 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 α7β2 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-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-100856R
-
|
|
PTHR
Reference Standards
|
Endocrinology
|
|
PCO371 (Standard) is the analytical standard of PCO371 (HY-100856). This product is intended for research and analytical applications. PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
|
-
- HY-10629R
-
|
WAY 252623 (Standard)
|
Reference Standards
LXR
|
Metabolic Disease
Cancer
|
|
LXR-623 (Standard) is the analytical standard of LXR-623. This product is intended for research and analytical applications. LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
|
-
- 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-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-10233R
-
|
Lu 02-030 hydrochloride (Standard); THIP hydrochloride (Standard)
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. 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 .
|
-
- 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 α7β2 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-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) .
|
-
- 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-101300R
-
|
LD 3098 hydrochloride (Standard)
|
Reference Standards
Adenosine Receptor
|
Neurological Disease
|
|
Cirazoline (hydrochloride) (Standard) is the analytical standard of Cirazoline (hydrochloride). This product is intended for research and analytical applications. 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) .
|
-
- HY-A0007R
-
|
N-0923 Hydrochloride (Standard)
|
Reference Standards
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-123942
-
Diprovocim
Maximum Cited Publications
14 Publications Verification
|
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-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 . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
|
-
- HY-B0584R
-
|
Fluprostenol isopropyl ester(Standard); AL6221(Standard); Flu-Ipr (Standard)
|
Reference Standards
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-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-B0659AR
-
|
UK 14304 tartrate (Standard); AGN190342 tartrate (Standard)
|
Reference Standards
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-W399025
-
|
|
Opioid Receptor
Arrestin
|
Neurological Disease
|
|
ID110460001 is a full agonist of μ-opioid receptor and an agonist of δ-opioid receptor. ID110460001 exhibits high intrinsic efficacy for G protein pathway activation of μ-opioid receptor, and this property is not affected by the reduction in receptor quantity. ID110460001 acts only as a very weak partial agonist in the β-arrestin-2 pathway of both receptors, and binds to μ-opioid receptor via a specific mode. The efficacy of ID110460001 in the G protein pathway of δ-opioid receptor is sensitive to changes in receptor quantity. ID110460001 can be used in pain-related research .
|
-
- 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-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-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-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-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-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-15394R
-
|
N-0437 hydrochloride (Standard)
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
Reference Standards
|
Neurological Disease
Endocrinology
|
|
(Rac)-Rotigotine (hydrochloride) (Standard) is the analytical standard of (Rac)-Rotigotine (hydrochloride). This product is intended for research and analytical applications. (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-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-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-P3057
-
-
- HY-B0584S2
-
|
Fluprostenol isopropyl ester-7; AL6221-7; Flu-Ipr-7
|
Isotope-Labeled Compounds
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Travoprost-d7 (Fluprostenol isopropyl ester-d7) is deuterium labeled Travoprost. 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-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-125055A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
CD08108 is a selective MC1R full agonist with an EC50 of 70 nM against hMC1R. CD08108 participates in the melanogenesis process. CD08108 promotes cell proliferation. CD08108 can be used in studies related to vitiligo, subcutaneous diseases and photosensitive diseases .
|
-
- HY-100428
-
|
MCC-555; Isaglitazone
|
PPAR
|
Metabolic Disease
|
|
Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus .
|
-
- 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-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-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-B1532
-
|
(S)-Anabasine; (+)-Anabasine
|
Environmental Pollutants
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-182473
-
|
|
Prostaglandin Receptor
|
Neurological Disease
|
|
AL-6556 is a full agonist of the DP receptor and a partial agonist of the EP2 receptor. AL-6556 has an EC50 of 799 nM for bovine DP, a Ki of 3200 nM for human DP, and an EC50 of 1180 nM for human EP2, with selectivity over EP3, FP, IP, TP and 19 non-prostaglandin receptors. AL-6556 stimulates cAMP production via receptor activation and reduces intraocular pressure through aqueous humor inflow and outflow mechanisms. AL-6556 can be used in research related to ocular hypertension and glaucoma .
|
-
- HY-107678R
-
|
WAY-317538 (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
|
|
SEN12333 (Standard) is the analytical standard of SEN12333 (HY-107678). This product is intended for research and analytical applications. 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 Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
|
-
- 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-185356
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SR-14968 is a full, allosteric and non-competitive MOR agonist, with an EC50 of 88 nM for MOR in mouse brainstem. SR-14968 stabilizes MOR in a G protein signaling state that is resistant to washout but reversible by antagonists. SR-14968 induces respiratory depression in mice. SR-14968 can be used in pain-related research .
|
-
- 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-10680R
-
|
|
Reference Standards
GPR109A
|
Cancer
|
|
MK-6892 (Standard) is the analytical standard of MK-6892 (HY-10680). This product is intended for research and analytical applications. 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-P11469
-
-
- HY-101299A
-
|
DAR-0100
|
Dopamine Receptor
YAP
|
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-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-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-100428R
-
|
MCC-555 (Standard); Isaglitazone (Standard)
|
Reference Standards
PPAR
|
Metabolic Disease
|
|
Netoglitazone (Standard) is the analytical standard of Netoglitazone (HY-100428). This product is intended for research and analytical applications. Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus .
|
-
- 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-100658
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
|
-
- HY-113413
-
|
Imidazolyl-4-acetic acid
|
Endogenous Metabolite
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
|
-
- HY-B1532R
-
|
(S)-Anabasine (Standard); (+)-Anabasine (Standard)
|
Reference Standards
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-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-145604
-
|
RG7774
|
Cannabinoid Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Vicasinabin (RG7774) is an orally active, selective, and full CB2R agonist, with EC50 values of 2.81 nM and 2.60 nM for human CB2R and mouse CB2R, respectively. Vicasinabin inhibits inflammation, reduces leukocyte adhesion and decreases vascular permeability by selectively activating CB2R. Vicasinabin can be used in the researches for diabetic retinopathy, uveitis and laser-induced choroidal neovascularization .
|
-
- 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-103231
-
|
|
iGluR
|
Neurological Disease
|
|
(S)-CPW 399 is a subtype-selective full agonist of AMPA receptors, with a 20-fold higher selectivity for GluA1 and GluA2 subunits over GluA3 and GluA4 subunits. (S)-CPW 399 can significantly increase the spontaneous firing rate (FR) of LC noradrenergic neurons by activating AMPA receptors containing GluA1 subunits. (S)-CPW 399 can be used for the study of neurological diseases .
|
-
- 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-100658S
-
|
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
|
-
- HY-129481
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 178210 (Compound 24) is a selective partial agonist of the 5-HT1A receptor, with Ki values of 0.67 and 380 nM for the 5-HT1A and 5-HT1D receptors, respectively. LY 178210 has almost no activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors. LY 178210 inhibits Foscolin-stimulated cyclase activity, but its maximum potency is lower than that of the full agonist 8-OH-DPAT (HY-112061). LY 178210 significantly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the greater hypothalamus and increases serum corticosterone concentrations .
|
-
- 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-101299BR
-
|
DAR-0100 hydrochloride (Standard)
|
Dopamine Receptor
Reference Standards
|
Neurological Disease
|
|
Dihydrexidine (hydrochloride) (Standard) is the analytical standard of Dihydrexidine (hydrochloride) (HY-101299B). This product is intended for research and analytical applications. 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-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-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-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-154980
-
|
|
GPR52
|
Neurological Disease
|
|
NXE0041178 is an orally active and BBB-penetrant full GPR52 agonist, with a pEC50 of 7.5 for human GPR52 and an EC50 of 27.5 nM (pEC50 = 7.55) for rat GPR52. NXE0041178 shows no significant inhibition on hERG, hNaV1.5 and cytochrome P450 isoforms. NXE0041178 can reduce d-amphetamine-induced hyperactivity in rats. NXE0041178 can be used for research of Neurological disease .
|
-
- 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-100658R
-
|
|
5-HT Receptor
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
|
-
- HY-B0188A
-
|
Org GB 94
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-113413R
-
|
Imidazolyl-4-acetic acid (Standard)
|
Reference Standards
Endogenous Metabolite
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
|
-
- 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) .
|
-
- HY-B0188
-
|
Mianserine
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-120493A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AM-6226 is a potent and orally active G protein coupled receptor 40 (GPR40) full agonist with an EC50 of 0.12 μM. AM-6226 can activate the GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promote insulin secretion in a glucose-dependent manner and also increase the release of incretin hormones (GLP-1, GIP), thereby avoiding the risk of hypoglycemia. AM-6226 can be used for the research of metabolic disease, such as diabetes .
|
-
- HY-118504
-
|
|
Environmental Pollutants
nAChR
|
Neurological Disease
|
|
Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
|
-
- 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-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-14296A
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
PF-610355 hydrochloride is a β2-adrenergic receptor (β2-AR) full agonist with selectivity for β1-adrenergic receptors. PF-610355 hydrochloride increases intracellular cAMP levels, induces sustained tracheal smooth muscle relaxation, and inhibits acetylcholine-induced bronchoconstriction. PF-610355 hydrochloride can be used in research related to chronic obstructive pulmonary disease, asthma, and respiratory system diseases .
|
-
- HY-10435AR
-
|
(±)-SKF-82958 hydrobromide (Standard); Chloro-APB hydrobromide (Standard)
|
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 (hydrobromide) (Standard) is the analytical standard of SKF-82958 (hydrobromide). This product is intended for research and analytical applications. 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-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-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-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-118504S
-
|
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
|
|
Sulfoxaflor-d3 is the deuterium labeled Sulfoxaflor (HY-118504). Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
|
-
- HY-135581S1
-
|
|
Isotope-Labeled Compounds
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 .
|
-
- 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-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. . 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-13467
-
AM-1638
3 Publications Verification
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AM-1638 is an orally active full agonist of GPR40 (EC50: 0.16 μM). AM-1638 increases the expression of antioxidant molecules (HO-1 and NQO-1). AM1638 blocks Palmitate (HY-N0830)-mediated superoxide production and ER stress. AM-1638 has antidiabetic activity and improves glycemic control in BDF mice with diet-induced obesity (DIO). AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%) .
|
-
- 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-B0188AS
-
|
Org GB 94-d3
|
Isotope-Labeled Compounds
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-180181
-
|
|
RAR/RXR
|
Metabolic Disease
Cancer
|
|
RXR antagonist 6 (Compound 34) is a selective partial retinoid X receptor (RXR) antagonist. RXR antagonist 6 shows no agonistic activity for any of the human RXRα/β/γ subtypes but it can strongly inhibit the receptor activation induced by full agonists of RXR (such as Bezafibrate (HY-B0637)) with an IC50 of 2.7 μM. RXR antagonist 6 can enhance PMA (HY-18739)-induced THP-1 cell differentiation. RXR antagonist 6 can be used for the research of cancer, metabolic and neurological disease, such as lymphoma .
|
-
- HY-B0188AR
-
|
Org GB 94 (Standard)
|
Reference Standards
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- 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 .
|
-
- HY-120493
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
(rel)-AM-6226 is the relative stereoisomer of AM-6226 (HY-120493A). AM-6226 is a potent, orally active full agonist of G protein-coupled receptor 40 (GPR40) with an EC50 value of 0.12 μM. AM-6226 activates GPR40 receptors on pancreatic β-cells and enteroendocrine L-cells, promotes insulin secretion in a glucose-dependent manner, and increases the release of incretin hormones (GLP-1, GIP), thus avoiding the risk of hypoglycemia. AM-6226 can be used in the research of metabolic diseases such as diabetes .
|
-
- HY-W686762
-
|
|
Dopamine Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
m,p-Dimethyl PPE is a D4 dopamine receptor ligand. m,p-Dimethyl PPE promotes GDP/GTP exchange of the G protein α-subunit, dissociates the receptor-G protein complex, stabilizes the low-affinity receptor state, and inhibits adenylate cyclase activity. m,p-Dimethyl PPE inhibits Forskolin (HY-15371)-induced melatonin synthesis in retinal photoreceptor cells and reduces the efficacy of full agonists when used in combination. m,p-Dimethyl PPE can be used in studies related to attention-deficit hyperactivity disorder .
|
-
- HY-B0188S
-
|
Mianserine-d3
|
Histamine Receptor
Isotope-Labeled Compounds
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-106993AR
-
|
GT-2331 maleate (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant maleate (Standard) is the analytical standard of Cipralisant (maleate) (HY-106993A). This product is intended for research and analytical applications. 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-148596
-
|
UDP-N-Acetyl-D-glucosamine; Uridine diphospho-N-acetylglucosamine; UDP-N-acetylglucosamine
|
Endogenous Metabolite
P2Y Receptor
Drug Intermediate
Glycosyltransferase
|
Infection
|
|
UDP-GlcNAc (UDP-N-Acetyl-D-glucosamine) is an important component and precursor of bacterial peptidoglycan. UDP-GlcNAc is a nucleotide sugar used by Glycosyltransferases to synthesize glycoproteins, glycosaminoglycans, glycolipids, and glycoRNA. UDP-GlcNAc also serves as the donor substrate for forming O-GlcNAc, a dynamic intracellular protein modification involved in diverse signaling and disease processes. UDP-GlcNAc is the sugar nucleotide donor for the synthesis of O-GlcNAc modified proteins. UDP-GlcNAc also acts as a full agonist of the P2Y14 receptor and inhibits the formation of cAMP. UDP-GlcNAc can be used in studies related to bacterial infections .
|
-
- HY-106432A
-
|
SB-202026 hydrochloride; Memric hydrochloride
|
mAChR
Dopamine Receptor
|
Neurological Disease
|
|
Sabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pKi=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases .
|
-
- HY-180398
-
|
|
PPAR
PGC-1α
|
Metabolic Disease
|
|
PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes .
|
-
- HY-107581
-
MK-1903
1 Publications Verification
|
GPR109A
MMP
|
Metabolic Disease
Inflammation/Immunology
|
|
MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases .
|
-
- HY-106993R
-
|
GT-2331 (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant (Standard) (GT-2331 (Standard)) is the analytical standard of Cipralisant (HY-106993). This product is intended for research and analytical applications. 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-107581R
-
|
|
Reference Standards
GPR109A
MMP
|
Metabolic Disease
Inflammation/Immunology
|
|
MK-1903 (Standard) is the analytical standard of MK-1903 (HY-107581). This product is intended for research and analytical applications. MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases.
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- 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-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-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-P0076
-
TAK-448
3 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-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-P2197
-
-
- 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-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-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-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-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-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-P5131
-
|
|
Opioid Receptor
|
Others
|
|
[Dmt1]DALDA is a potent and long-acting analgesic binds to the mu opioid receptor with high affinity and selectivity. [Dmt1]DALDA is a full agonist at hMOR (Kd = 0.199 nM) and hDOR, but only partial agonist against hKOR .
|
-
- HY-P3876
-
-
- 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-P11469
-
-
- 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-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-P3057
-
-
- 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-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-P11810
-
|
|
GnRH Receptor
Neuropeptide FF Receptor
|
Metabolic Disease
|
|
GUB08248 is a full GPR10 agonist and a partial NPFF2R agonist, with EC50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 inhibits food intake and induces sustained weight loss. GUB08248 can be used in obesity-related research .
|
-
- HY-P11432
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
PG-911 is a full MC5R agonist (EC50 = 0.031 nM for hMC5R). PG-911 is also a full antagonist at the hMC3R and the hMC4R (Kb: 0.38 nM and 0.17 nM, respectively). PG-911 can be used in the research of neurological disorders .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- 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-B0659S
-
|
|
|
Brimonidine-d4 is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
|
-
-
- HY-B0188S
-
|
|
|
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-15394S
-
|
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(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.
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- HY-B0188AS
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Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-W743727
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Cytisine-d4 is the deuterium labeled Cytisinicline (HY-N0175). 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-10019S2
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Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. 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 α7β2 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-10019S1
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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 α7β2 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-10020S
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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 .
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- HY-A0095S
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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) .
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- HY-10019S
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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 . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
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- HY-15394S1
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(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.
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- HY-10019AS1
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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 .
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- HY-B0584S2
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Travoprost-d7 (Fluprostenol isopropyl ester-d7) is deuterium labeled Travoprost. 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-A0095S1
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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) .
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- HY-118504S
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Sulfoxaflor-d3 is the deuterium labeled Sulfoxaflor (HY-118504). Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
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- HY-135581S1
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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 .
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- HY-135582S1
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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. . 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 .
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- HY-135582S
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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 .
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- HY-100658S
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Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
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- HY-128855
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Alkynes
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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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