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Search Results for " desensitization "

ターゲット

12

阻害剤

1

天然化合物

7

リコンビナントタンパク質

カタログ番号 製品名 別名 ターゲット
T4573 Cyclothiazide GluR
Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).
T14989 CMPD101 ROCK , GRK , PKC
CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with I...
T4236 AR-M 1000390 hydrochloride ARM390 Hydrochloride,ARM-390 HCl Opioid Receptor
AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic resp...
T27806 Lecozotan HCl SRA-333,SRA333,SRA 333,Lecozotan hydrochloride 5-HT Receptor
Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. ...
T33289 Meproadifen
Meproadifen enhances activation and desensitization of the acetylcholine receptor-ionic channel complex (AChR).
TP2058 Catestatin
Non-competitive nicotinic cholinergic antagonist; selectively inhibits nicotinic-stimulated catecholamine secretion from chromaffin cells and noradrenergic neurons (IC50 ~ 200 nM). Blocks nicotinic-induced cationic signa...
T38392 JAMI1001A
JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both flip and flop receptor isoforms.
T36634 ZQ 16
Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK...
T80503 Proadrenomedullin (N-20) (bovine, porcine) ProADM N20(bovine, porcine),PAMP-20(bovine, porcine)
Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a peptide known for its strong hypotensive effects and inhibition of catecholamine release from chromaffin cells without competing with other substances. It effe...
T76399 PKI(5-22)amide
PKI(5-22)amide, an active inhibitory fragment of the cyclic AMP-dependent protein kinase (PKA) inhibitor, effectively prevents PKA activation. However, it does not reduce the homologous desensitization of CRF1 receptors ...
T72744 (R)-PF-06256142
(R)-PF-06256142, the R enantiomer of PF-06256142, exhibits low activity. PF-06256142 itself is distinguished as a potent and selective orthosteric D1 receptor agonist, with the capability to minimize receptor desensitiza...
T71398 RO5126946
RO5126946 is a Novel α7 nicotinic acetylcholine receptor-positive allosteric modulator. RO5126946 allosterically modulates α7nAChR activity. RO5126946 increased acetylcholine-evoked peak current and delayed current decay...
カタログ番号 製品名 別名 ターゲット
TN5580 Rediocide A
Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediate...

Recombinant Proteins

カタログ番号 製品名 Species Expression System
TMPJ-00983 ARRB1 Protein, Human, Recombinant (His) Human E. coli
β-Arrestin-1 (ARRB1) is a cytoplasmic protein that belongs to the arrestin family. ARRB1 is expressed at high levels in peripheral blood leukocytes and the central nervous system. ARRB1 regulates agonist-mediated G-prote...
TMPH-02267 AGTRAP Protein, Human, Recombinant (His & Myc & SUMO) Human in vitro E. coli expression system
Appears to be a negative regulator of type-1 angiotensin II receptor-mediated signaling by regulating receptor internalization as well as mechanism of receptor desensitization such as phosphorylation. Induces also a decr...
TMPH-02331 GLRA1 Protein, Human, Recombinant (His & Myc) Human E. coli
Glycine receptors are ligand-gated chloride channels. Channel opening is triggered by extracellular glycine. Channel opening is also triggered by taurine and beta-alanine. Channel characteristics depend on the subunit co...
TMPY-04555 GRK5 Protein, Human, Recombinant (His) Human Baculovirus-Insect Cells
G protein-coupled receptor kinase 5, also known as G protein-coupled receptor kinase GRK5 and GRK5, is a member of the protein kinase superfamily, AGC Ser/Thr protein kinase family, and GPRK subfamily. GRKs specifically ...
TMPH-02540 GRK2 Protein, Mouse, Recombinant (His & SUMO) Mouse E. coli
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to...
TMPH-01719 OPRM1 Protein, Human, Recombinant (His) Human in vitro E. coli expression system
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to th...
TMPJ-00715 FGF-19 Protein, Human, Recombinant (His) Human E. coli
Fibroblast growth factor 19 (FGF19) is a secreted protein which belongs to the FGFs family. FGF19 is expressed in fetal brain, cartilage, retina, and adult gall bladder. FGFs modulate cellular activity via at least 5 dis...