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カタログ番号 | 製品名 | 別名 | ターゲット |
---|---|---|---|
T8423 | ML417 | Dopamine Receptor , Arrestin | |
ML417 is a selective and brain penetrant agonist of D3 Dopamine (EC50 : 38 nM). | |||
T21874 | CID 2745687 | GPR | |
CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site. | |||
T26869 | BMS-986122 | BMS 986122 | Opioid Receptor |
BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC5... | |||
T28073 | MLS1547 | MLS000051547,MLS 1547,MLS-1547 | Dopamine Receptor |
MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assa... | |||
T15183 | Dynarrestin | Hedgehog/Smoothened | |
Dynarrestin is an inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells. It inhibits dynein 1-driven microtubule gliding in vitro pl... | |||
T12006 | Metarrestin | ML246 | DNA/RNA Synthesis |
Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (... | |||
T61562 | CB1R Allosteric modulator 3 | cAMP , Cannabinoid Receptor | |
CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction. | |||
T23434 | GPR35 agonist 2 | TC-G 1001 | GPR , Arrestin |
GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively. | |||
T33452 | ML192 | ML-192,CID1434953,CID 1434953,ML 192,CID-1434953 | Cannabinoid Receptor , GPR , Arrestin |
ML192 (CID1434953) is a selective GPR55 ligand antagonist. ML192 is an inhibitor that inhibits β-arrestin transport, ERK1/2 phosphorylation, and PKCβII translocation. | |||
TP2158L1 | TRV-120027 acetate (1234510-46-3 free base) | RAAS , Arrestin | |
TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling. | |||
TP2158 | TRV-120027 TFA | TRV-120027 TFA (1234510-46-3 free base) | RAAS , Arrestin |
TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling. | |||
TP1923L1 | ELA-14(human) acetate | ELA-14(human) acetate (1886973-05-2 free base) | Apelin receptor , Arrestin |
ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide. | |||
T4390 | ML221 | Apelin receptor , Arrestin | |
ML221 is a potent apelin /APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. | |||
T77673 | 7-FluorotryptaMine HCl | GPR , Arrestin | |
7-FluorotryptaMine HCl is a potent aromatic monoamine GPRC5A agonist that induces GPRC5A-mediated β-arrestin recruitment.7-FluorotryptaMine HCl can be used to study signalling pathways related to immunity and cancer. | |||
TP1922L1 | ELA-11 (human) acetate(1784687-32-6 free base) | Apelin receptor , Arrestin | |
ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. | |||
TP2112L | TC14012 acetate | TC14012 acetate(368874-34-4 free base) | CXCR , Arrestin |
TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrest... | |||
T41231 | GP 1a | Cannabinoid Receptor , PERK , Arrestin | |
GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and incr... | |||
T33613 | NCGC00135472 | NCGC 00135472,DRV1 (GPR32) agonist C2A,C2A,NCGC-00135472 | Others |
NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1/GPR32 receptor in beta-blocker and cAMP assays ... | |||
T29065 | UNC9994 | UNC-9994,UNC 9994 | |
UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities. | |||
T29061 | UNC0006 | UNC 0006,UNC-0006 | |
UNC0006 is a β-arrestin-biased dopamine D2 ligand. | |||
T29064 | UNC9975 | UNC-9975 | |
UNC9975 is an analog of aripiprazole and a β-arrestin-biased D2R agonist. | |||
T29066 | UNC9995 | UNC-9995,UNC 9995 | |
UNC9995 is a β-Arrestin-Biased Dopamine D2 Receptor agonist (β-Arrestin, EC50 = 120 nM; Emax = 88%). | |||
T70040 | BRD5814 | ||
BRD5814 is a highly brain penetrant β-arrestin biased D2R antagonist. | |||
T10926 | CYT-1010 | Others | |
CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively. | |||
T23866 | CCX777 | CCX 777,CCX-777 | Arrestin |
CCX777 is a partial agonist recruited to ACKR3 by β-arrestin-2 and is used in cancer research. | |||
T37304 | 5-OxoETE methyl ester | ||
5-OxoETE methyl ester is an esterified form of the polyunsaturated keto acid 5-oxoETE . 5-OxoETE methyl ester is an agonist of oxoeicosanoid receptor 1 (OXER1; EC50 = 1.54 μM for β-arrestin recruitment) that has a higher... | |||
T79312 | FGH31 | Dopamine Receptor | |
FGH31 (Compound 24), a dopamine D4 agonist, exhibits potent and selective GRK2-dependency with a K i of 1.6 nM and partially activates β-arrestin [1]. | |||
T70342 | MRS542 | ||
MRS542 is a A3AR antagonist as found by cyclic AMP assays, and a partial agonist as found by beta-arrestin translocation. LUF6000 is responsible for the partial agonist nature of MRS542. | |||
T79744 | GPR55 agonist 4 | ||
GPR55 agonist 4 (Compound 28), with an EC50 of 131 nM for hGPR55 and 1.41 nM for rGPR55, effectively induces β-arrestin recruitment to human GPR55 [1]. | |||
T64305 | APJ receptor agonist 7 | ||
APJ receptor agonist 7 (compound 37) is an orally active APJ (apelin receptor) agonist (Ki: 0.059 μM). arrestin (EC50: 0.063 μM). | |||
T10926L | CYT-1010 hydrochloride | Others | |
CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively. | |||
T62853 | UNC9994 hydrochloride | ||
UNC9994 hydrochloride is a functionally selective, β-arrestin-biased dopamine D2 receptor (D2R) agonist (Ki: 79 nM) that selectively activates β- arresttin recruitment and signal transduction. UNC9994 hydrochloride is a ... | |||
T61964 | RXFP3/4 agonist 2 | RXFP receptor | |
RXFP3/4 agonist 2 is a potent non-peptidic bis-RXFP3/4 agonist that induces the interaction between RXFP3 and β-arrestin-2, and can be used to study diseases caused by metabolic abnormalities. | |||
T78735 | D1R antagonist 1 | Dopamine Receptor | |
Compound 12a (D1R antagonist 1) is a D1R antagonist that participates in both G-protein-coupled and β-arrestin-mediated signaling pathways [1]. | |||
T78736 | D3R ligand 1 | Dopamine Receptor | |
D3R Ligand 1 (compound 23b) is a potent, selective antagonist of the dopamine D3 receptor (Ki=66 nM), incorporating a THPB template. It inhibits both G-protein- and β-arrestin-mediated signaling pathways [1]. | |||
T10716 | CCR7 Ligand 1 | CCR7-Cmp2105 | Others |
T61371 | CB1R Allosteric modulator 4 | ||
CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arresti... | |||
T80140 | (Val3,Pro8)-Oxytocin | Oxytocin Receptor | |
(Val3,Pro8)-Oxytocin functions primarily as a Gq-dependent pathway agonist and exhibits secondary activity as a reduced efficacy agonist for β-arrestin recruitment and receptor-mediated endocytosis at the oxytocin recept... | |||
TP1922 | ELA-11(human) | ELA-11 (human) | |
High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. | |||
TP2158L | TRV-120027 | Others | |
TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. | |||
T68247 | PSB-KD107 | ||
PSB-KD107 is an agonist of the Cannabinoid-Activated Orphan G‑Protein-Coupled Receptor GPR18. PSB-KD107 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment... | |||
T73690 | Abaloparatide | ||
Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs/cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in... | |||
T76053 | ELA-11(human) TFA | ||
ELA-11(human) TFA, a bioactive fragment of ELA-32, acts as a high-affinity apelin receptor agonist (K i =14 nM). It effectively inhibits forskolin-induced cAMP production and promotes β-arrestin recruitment in vitro, hig... | |||
TP2141 | Balixafortide TFA (1051366-32-5 free base) | Balixafortide TFA,POL6326 TFA | CXCR |
Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-... | |||
TP1923 | Elabela(19-32) | ELA-14 (human) | |
Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo. | |||
T79721 | GPR55 agonist 3 | ||
Compound 26, a GPR55 agonist, exhibits potent activity with EC50 values of 0.239 nM for hGPR55 and 1.76 nM for rGPR55. It also induces β-arrestin recruitment to human GPR55 with an EC50 of 6.2 nM [1]. | |||
T76044 | Elabela(19-32) TFA | ||
Elabela(19-32) TFA, an effective fragment of ELABELA (ELA), selectively engages with the apelin receptor (APJ). This compound initiates G αi1 and β-arrestin-2 signaling, demonstrating EC50 values of 8.6 nM and 166 nM, re... | |||
T73665 | Bufrolin | ||
Bufrolin, an analog of Cromoglycate (histamine release inhibitor) and a potent agonist of GPR35, enhances the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. It stabilizes mast cells, exhibiting ant... | |||
T36923 | CXCR2-IN-2 | CXCR2-IN-2 | |
CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-f... | |||
TP2096 | ELA-21 (human) | ||
High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inh... |
カタログ番号 | 製品名 | Species | Expression System |
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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-00299 | Rhodopsin Protein, Bovine, Recombinant (His) | Bovine | E. coli |
Photoreceptor required for image-forming vision at low light intensity. Required for photoreceptor cell viability after birth. Light-induced isomerization of 11-cis to all-trans retinal triggers a conformational change t... | |||
TMPH-03123 | Rhodopsin Protein, Pig, Recombinant (GST & His) | Sus scrofa (Pig) | E. coli |
Photoreceptor required for image-forming vision at low light intensity. Required for photoreceptor cell viability after birth. Light-induced isomerization of 11-cis to all-trans retinal triggers a conformational change t... | |||
TMPH-03124 | Rhodopsin Protein, Pig, Recombinant (GST) | Sus scrofa (Pig) | E. coli |
Photoreceptor required for image-forming vision at low light intensity. Required for photoreceptor cell viability after birth. Light-induced isomerization of 11-cis to all-trans retinal triggers a conformational change t... | |||
TMPH-03265 | CMKLR2 Protein, Rat, Recombinant (His) | Rat | E. coli |
Receptor for chemoattractant adipokine chemerin/RARRES2 suggesting a role for this receptor in the regulation of inflammation and energy homesotasis. Signals mainly via beta-arrestin pathway. Binding of RARRES2 activates... | |||
TMPH-00300 | Rhodopsin Protein, Bovine, Recombinant (His & KSI) | Bovine | E. coli |
Photoreceptor required for image-forming vision at low light intensity. Required for photoreceptor cell viability after birth. Light-induced isomerization of 11-cis to all-trans retinal triggers a conformational change t... | |||
TMPJ-00952 | CXCL12 Protein, Mouse, Recombinant | Mouse | E. coli |
Mouse Cxcl12 is a secreted and highly conserved protein which belongs to the intercrine alpha (chemokine CxC) family.CXCL12 is widely expressed in various organs including brain, kidney, skeletal muscle, heart, liver, an... |