Search Result
Results for "
Gq
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-125791
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Succinate Receptor 1
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Cardiovascular Disease
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cis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 μM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system .
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- HY-15523
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CMV
DNA/RNA Synthesis
G-quadruplex
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Cancer
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Braco-19 is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor .
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- HY-W013724
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IDP disodium; Inosine-5'-diphosphoric acid disodium
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c-Myc
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Inosine-5'-diphosphate disodium (IDP disodium) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate disodium has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate disodium abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate disodium has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate disodium can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
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- HY-P3137
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Angiotensin Receptor
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Cardiovascular Disease
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TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .
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- HY-111254
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PPAR
NF-κB
JNK
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Inflammation/Immunology
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GQ-16 is an orally active PPARγ partial agonist with an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer .
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- HY-107111
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mAChR
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Neurological Disease
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GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-15523A
-
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DNA/RNA Synthesis
CMV
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Infection
Cancer
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Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor .
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- HY-169841
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5-HT Receptor
Arrestin
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Neurological Disease
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IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT2AR with a Ki of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression .
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- HY-121675
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BOL-148; Bromolysergide
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5-HT Receptor
G protein-coupled Bile Acid Receptor 1
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Neurological Disease
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2-Bromo-LSD (BOL-148) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD lacks 5-HT2B agonist activity. 2-Bromo-LSD induces dendritogenesis and spinogenesis. 2-Bromo-LSD reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
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- HY-149101
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IDP; Inosine-5'-diphosphoric acid
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c-Myc
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
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- HY-164795
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
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SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
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- HY-164795A
-
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
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SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
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- HY-134807
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P2X Receptor
5-HT Receptor
Autophagy
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Cancer
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Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
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- HY-P6292
-
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PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
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Neurological Disease
Cancer
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KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
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- HY-42346
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- HY-W747599
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Tetrasialoganglioside Gq1b sodium
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Pyk2
Endogenous Metabolite
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Neurological Disease
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Ganglioside GQ1b (bovine) sodium promotes neurite outgrowth during early neuronal differentiation. Ganglioside GQ1b (bovine) sodium controls the neuronal differentiation process in mESCs .
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- HY-114933
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mAChR
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Neurological Disease
Metabolic Disease
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VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity .
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- HY-111763
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- HY-P2381
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Angiotensin Receptor
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Others
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Sar-Arg-Val-Tyr-Val-His-NH2 is a Gq-biased agonists, exhibits 10-fold larger molecular efficacies at the AT1R-Gq fusion protein compared with the AT1R-βarr2 fusion protein .
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- HY-P10365
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Adhesion G Protein-coupled Receptors (AGPCRs)
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Others
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Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members .
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- HY-160001A
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- HY-176921
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Leukotriene Receptor
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Inflammation/Immunology
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ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC50 = 14 nM). ONO-2570366 inhibits the binding of LTD4Gq signaling pathway mediated by receptor activation. ONO-2570366 can be used for the researches of inflammation and immunology, such as asthma .
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- HY-P5358
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Protease Activated Receptor (PAR)
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Others
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YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
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- HY-175515
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5-HT Receptor
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Neurological Disease
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5-HT2C agonist-11 (Compound 1) is an orally active, brain-penetrant and selective 5-HT2C receptor agonist (EC50=15 nM). 5-HT2C agonist-11 activates the Gq protein signaling pathway, promoting intracellular calcium release. 5-HT2C agonist-11 is promising for research of depression, post-traumatic stress disorder (PTSD) and neuropathic pain .
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- HY-P11540
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Cholecystokinin Receptor
MMP
Amyloid-β
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Neurological Disease
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CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease .
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- HY-138951
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- HY-114865
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RGS Protein
Calcium Channel
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Neurological Disease
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BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux .
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- HY-156532C
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5-HT Receptor
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Neurological Disease
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(-)-5-HT2C agonist-3 (compound (-)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .
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- HY-173003
-
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Mas-related G-protein-coupled Receptor (MRGPR)
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Inflammation/Immunology
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EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC50 for Gq being 211.6 nM .
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- HY-157955
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- HY-179008
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5-HT Receptor
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Neurological Disease
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5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT2CR agonist, with an EC50 of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity .
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- HY-121140
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Free Fatty Acid Receptor
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Metabolic Disease
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AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .
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- HY-160001
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- HY-RS22188
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Small Interfering RNA (siRNA)
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Others
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Gnaq Mouse Pre-designed siRNA Set A contains three designed siRNAs for Gnaq gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Gnaq Mouse Pre-designed siRNA Set A
Gnaq Mouse Pre-designed siRNA Set A
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- HY-111273
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- HY-182405
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Apoptosis
YAP
ERK
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Cancer
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GQ127 is an orally active Gαq/11 inhibitor with an IC50 of 22.6 μM. GQ127 binds directly to Gαq/11 protein and inhibits its activity. GQ127 induces Apoptosis, suppresses viability, migration and invasion of uveal melanoma cells. GQ127 increases the phosphorylation level of YAP and decreases the phosphorylation level of ERK. GQ127 inhibits the growth of uveal melanoma xenografts in mouse models. GQ127 can be used for research related to uveal melanoma .
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- HY-107111A
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Cholinesterase (ChE)
mAChR
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Neurological Disease
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GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-P5017
-
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Oxytocin Receptor
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Endocrinology
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(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
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- HY-176141
-
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Trace Amine-associated Receptor (TAAR)
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Neurological Disease
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ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research .
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- HY-169791
-
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5-HT Receptor
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Neurological Disease
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ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors .
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- HY-P1432A
-
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GHSR
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Cancer
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K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
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- HY-137638
-
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PKA
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Metabolic Disease
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Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets .
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- HY-137638A
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Sp-5,6-DCI-cBIMPS
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PKA
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Metabolic Disease
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Sp-5,6-DCl-cBIMPS sodium is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS sodium stimulates insulin release. Sp-5,6-DCl-cBIMPS sodium inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets .
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- HY-W013724S
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IDP-15N4 dilithium; Inosine-5'-diphosphoric acid-15N4 disodium
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Isotope-Labeled Compounds
c-Myc
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
|
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Inosine-5'-diphosphate- 15N4 dilithium (IDP- 15N4 dilithium) is 15N labeled Inosine-5'-diphosphate dilithium. Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
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- HY-179843
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- HY-181878
-
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Z7149
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Serotonin Transporter
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .
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- HY-107111R
-
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Reference Standards
mAChR
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Neurological Disease
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GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-179541
-
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Drug Derivative
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Others
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PtdIns-(5)-P1-(1,2-dioctanoyl) ammonium is a synthetic phosphatidylinositol (PtdIns) derivative. PtdIns-(5)-P1-(1,2-dioctanoyl) ammonium can be used as a membrane phospholipid model in in vitro enzymology studies .
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- HY-179542
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Drug Derivative
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Others
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PtdIns-(4)-P1-(1,2-dihexanoyl) sodium is a synthetic phosphatidylinositol (PtdIns) derivative. PtdIns-(4)-P1-(1,2-dihexanoyl) sodium can be used as a membrane phospholipid model in in vitro enzymology studies .
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- HY-145156
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GLP Receptor
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Metabolic Disease
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CHU-128 is an effective and selective GLP-1R agonist. CHU-128 exhibits strong signal specificity and can activate the Gs/cAMP pathway, but it cannot activate the Gq/calcium signal, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 can be used for research on type 2 diabetes .
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- HY-121675A
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BOL-148 D-Tartrate; Bromolysergide D-Tartrate
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5-HT Receptor
G protein-coupled Bile Acid Receptor 1
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Neurological Disease
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2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
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- HY-179721
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Cholecystokinin Receptor
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Neurological Disease
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CCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway (EC50 = 0.27 nM), but has almost no activity on Gq and Gs signaling pathways. CCKBR agonist-2 shows no significant protective effect in the mouse Alzheimer's disease model, proving that the simple activation of the Gi signal pathway does not play a dominant role in the improvement of cognitive function .
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- HY-186169
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5-HT Receptor
Drug Derivative
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Neurological Disease
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R-MDDMA, 4-methylenedioxymethamphetamine (MDMA) analogue, is a 5-HT2A/5-HT2C receptor modulator. R-MDDMA shows antagonistic activity against 5-HT2A/5-HT2C with IC50 values of 642 and 137 nM, and also shows partial agonist activity with EC50 values of 24.5 and 14.4 nM, but does not activate 5-HT2B receptors. R-MDDMA promotes cortical neuron growth. R-MDDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDDMA can be used for the researches of post-traumatic stress disorder and depression .
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- HY-186170
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5-HT Receptor
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Neurological Disease
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R-MDMA, 4-methylenedioxymethamphetamine (MDMA) isomer, is a 5-HT2A/5-HT2C receptor antagonist with an IC50 of 629 and 61.4 nM. R-MDMA promotes cortical neuron growth. R-MDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDMA can be used for the researches of post-traumatic stress disorder and depression .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3137
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Angiotensin Receptor
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Cardiovascular Disease
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TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .
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- HY-P6292
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PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
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Neurological Disease
Cancer
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KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
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- HY-P2381
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Angiotensin Receptor
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Others
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Sar-Arg-Val-Tyr-Val-His-NH2 is a Gq-biased agonists, exhibits 10-fold larger molecular efficacies at the AT1R-Gq fusion protein compared with the AT1R-βarr2 fusion protein .
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- HY-P10365
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Adhesion G Protein-coupled Receptors (AGPCRs)
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Others
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Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members .
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- HY-P5358
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Protease Activated Receptor (PAR)
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Others
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YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
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- HY-P11540
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Cholecystokinin Receptor
MMP
Amyloid-β
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Neurological Disease
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CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease .
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- HY-138951
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- HY-P2382
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Peptides
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Others
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TRV120056 is a Gq-biased agonists, exhibits 10-fold larger molecular efficacies at the AT1R-Gq fusion protein compared with the AT1R-βarr2 fusion protein .
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- HY-P5017
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Oxytocin Receptor
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Endocrinology
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(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
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- HY-P1432A
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GHSR
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Cancer
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K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-149101
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IDP; Inosine-5'-diphosphoric acid
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Human Gut Microbiota Metabolites
Microorganisms
Endogenous metabolite
Source Classification
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c-Myc
Apoptosis
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Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W013724S
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Inosine-5'-diphosphate- 15N4 dilithium (IDP- 15N4 dilithium) is 15N labeled Inosine-5'-diphosphate dilithium. Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
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| Cat. No. |
Product Name |
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Classification |
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