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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
GTPγS activation
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "GTPγS activation" in MCE Product Catalog:
1
Target:
Research Areas:
1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
1
1 Cited Publications
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BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
1
1 Cited Publications
Synonyms: SR57746A; SR57746 hydrochloride
Target:
5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK
Research Areas:
Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
1
1 Cited Publications
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Research Areas:
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
1
1 Cited Publications
Target:
Research Areas:
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
Synonyms: Guanosine 5'-[γ-thio]triphosphate tetralithium
Target:
Research Areas:
GTPγS (Guanosine 5'-[γ-thio]triphosphate) tetralithium is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS tetralithium to couple with G- protein α, to study its effect on kinase activity. GTPγS tetralithium acts as a component of lysis buffer .
Cat. No.: HY-167856
CAS No.: 3034664-39-3
Target:
Research Areas:
RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
Cat. No.: HY-P10495A
Target:
Research Areas:
Target:
Research Areas:
ASN04885796 (compound IV) is an GPR17 activator with an EC50 of 2.27 nM for GPR17 induced GTPγS binding. ASN04885796 has neuroprotective property and can be used for research of neurological diseases .
Cat. No.: HY-170973
Target:
KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
Cat. No.: HY-P10495
CAS No.: 1778685-49-6
Target:
Cat. No.: HY-116088
CAS No.: 1345982-24-2
Target:
Research Areas:
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
Cat. No.: HY-103565R
CAS No.: 97075-46-2
Target:
Research Areas:
AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
Cat. No.: HY-103565AR
CAS No.: 83027-13-8
Target:
Research Areas:
AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
Target:
Research Areas:
MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [ 35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease .
Cat. No.: HY-116295A
Target:
Research Areas:
MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [ 35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease .
Cat. No.: HY-119820
CAS No.: 135354-02-8
Synonyms: SR57746A free base
Target:
Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK
Research Areas:
Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-137677
CAS No.: 37589-80-3
Synonyms: Guanosine 5'-[γ-thio]triphosphate
Target:
Research Areas:
GTPγS (Guanosine 5'-[γ-thio]triphosphate) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS to couple with G- protein α, to study its effect on kinase activity. GTPγS acts as a component of lysis buffer .
Cat. No.: HY-167856A
Target:
Research Areas:
RTI-122 dihydrochloride is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
Cat. No.: HY-14604R
CAS No.: 90494-79-4
Synonyms: SR57746A (Standard); SR57746 hydrochloride (Standard)
Research Areas:
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
