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Search Results for " biased "

ターゲット

41

阻害剤

1

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
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...
T23002 ML-335 Opioid Receptor
ML-335 is a μ-δ isomer-targeted agonist, a μOR-δOR-biased ligand that can serve as a scaffold for the development of unique types of (isomer-biased) drugs.ML-335 is a MOR (μ-opioid receptor)/DOR (δ-opioid receptor) heter...
T9596 AP1189 acetate Melanocortin Receptor
AP1189 acetate is a biased agonist at melanocortin 1 and melanocortin 3 receptors.
T7281 F-15599 5-HT Receptor
F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist(Ki : 3.4 nM).
T40508L TRV120056 acetate TRV120056 acetate (40678-47-5 Free base) Others
TRV120056 acetate is a Gq-biased agonist with 10-fold greater molecular efficiency on AT1R-Gq fusion proteins than AT1R-βarr2 fusion proteins.
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.
T16321 NI-42 Epigenetic Reader Domain
NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM). It also has excellent sele...
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.
T71946 ID110460003
ID110460003 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
T29064 UNC9975 UNC-9975
UNC9975 is an analog of aripiprazole and a β-arrestin-biased D2R agonist.
T71438 ID110460001
ID110460001 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
T71985 ID110460002
ID110460002 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
T40220 TRV055 TRV055
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
T70040 BRD5814
BRD5814 is a highly brain penetrant β-arrestin biased D2R antagonist.
T29061 UNC0006 UNC 0006,UNC-0006
UNC0006 is a β-arrestin-biased dopamine D2 ligand.
T69844 NLX-219
NLX-219 is a selective 5-HT1A receptor-biased agonists.
T70765 TRV0109101
TRV0109101 is a G protein-biased agonist of the µ-opioid receptor.
T40920 TRV056 TRV056
TRV056 is a Gq-biased agonist of the angiotensin II type 1 receptor (AT1R), demonstrating efficacy in stimulating Gq-mediated cellular signaling. It can serve as a foundation for the development of Gq-biased AT1R agonist...
T29066 UNC9995 UNC-9995,UNC 9995
UNC9995 is a β-Arrestin-Biased Dopamine D2 Receptor agonist (β-Arrestin, EC50 = 120 nM; Emax = 88%).
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.
TQ0075 ML314 Neurotensin Receptor
ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.
T76196 TRV055 hydrochloride
TRV055 hydrochloride, a Gq-biased ligand and G-protein-biased agonist of the angiotensin II receptor type 1 (AT1R), effectively stimulates cellular Gq-mediated signaling [1].
T37622 F13714 fumarate F13714 fumarate
F13714 fumarate, a selective biased agonist of the 5-HT1A receptor, exhibits antidepressant-like effects upon single administration in the mouse model of chronic mild stress[1].
T39870 5-HT7R antagonist 1 free base 5-HT7R antagonist 1 free base
5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT 7 R receptor, with a dissociation constant (K i) of 6.5 nM.
T39995 TRV120055 TRV120055
TRV120055, a Gq-biased agonist, demonstrates a 10-fold higher molecular efficacy when tested against the AT1R-Gq fusion protein in comparison to the AT1R-βarr2 fusion protein.
T40508 TRV120056
TRV120056 is a Gq-biased agonist that demonstrates a molecular efficacy ten times greater at the AT1R-Gq fusion protein than at the AT1R-βarr2 fusion protein.
T60790 5-HT7R antagonist 1
5-HT7R antagonist 1 is a G protein-biased antagonist with Ki of 6.5 nM for 5-HT 7R.
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.
T36946 PW0464 PW0464
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1]. PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R...
T41189 AY 254
AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-woun...
TP2000 MM 07
Apelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in...
T38716 SAR247799 SAR247799,S1P1 agonist 3
SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells a...
T37907 DL 175
Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bo...
T76224 NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
Compound 40, NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal), a macrocyclic analogue of Ape13, acts as a potent APJ agonist with a Ki of 5.7 nM. It demonstrates favorable Gα12-biased signaling and possesses an enhanced in vivo half-life...
T80471 α-Conotoxin MrIC
α-Conotoxin MrIC is a biased agonist selective for the α7 nicotinic acetylcholine receptor (nAChR), with activation contingent upon the presence of type II positive allosteric modulators, such as PNU120596. It is utilize...
TP1354 ATI-2341 TFA (1337878-62-2 free base) ATI-2341 TFA
ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activa...
T60597 UCSF678
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities versus the single commercial antagonist SB-699551. UCSF678 is a selective probe...
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 ...
T82233 HCAR2 agonist 1
HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory properties by reducing mRNA levels of pro-inflammatory cytokin...
T75721 ATI-2341 TFA
ATI-2341 is a potent, functionally selective allosteric agonist of the C-X-C chemokine receptor type 4 (CXCR4), acting as a biased ligand that prefers Gαi activation over Gα13. This compound activates the inhibitory hete...
T37199 Bilaid C
Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293...

Compounds

MLS1547
T28073
Synonym: MLS000051547,MLS 1547,MLS-1547
Target: Dopamine Receptor
ML-335
T23002
Synonym:
Target: Opioid Receptor
AP1189 acetate
T9596
Synonym:
Target: Melanocortin Receptor
F-15599
T7281
Synonym:
Target: 5-HT Receptor
TRV120056 acetate
T40508L
Synonym: TRV120056 acetate (40678-47-5 Free base)
Target: Others
TRV-120027 acetate (1234510-46-3 free base)
TP2158L1
Synonym:
Target: RAAS, Arrestin
NI-42
T16321
Synonym:
Target: Epigenetic Reader Domain
TRV-120027 TFA
TP2158
Synonym: TRV-120027 TFA (1234510-46-3 free base)
Target: RAAS, Arrestin
ID110460003
T71946
Synonym:
Target:
UNC9975
T29064
Synonym: UNC-9975
Target:
ID110460001
T71438
Synonym:
Target:
ID110460002
T71985
Synonym:
Target:
TRV055
T40220
Synonym: TRV055
Target:
BRD5814
T70040
Synonym:
Target:
UNC0006
T29061
Synonym: UNC 0006,UNC-0006
Target:
NLX-219
T69844
Synonym:
Target:
TRV0109101
T70765
Synonym:
Target:
TRV056
T40920
Synonym: TRV056
Target:
UNC9995
T29066
Synonym: UNC-9995,UNC 9995
Target:
UNC9994
T29065
Synonym: UNC-9994,UNC 9994
Target:
ML314
TQ0075
Synonym:
Target: Neurotensin Receptor
TRV055 hydrochloride
T76196
Synonym:
Target:
F13714 fumarate
T37622
Synonym: F13714 fumarate
Target:
5-HT7R antagonist 1 free base
T39870
Synonym: 5-HT7R antagonist 1 free base
Target:
TRV120055
T39995
Synonym: TRV120055
Target:
TRV120056
T40508
Synonym:
Target:
5-HT7R antagonist 1
T60790
Synonym:
Target:
TRV-120027
TP2158L
Synonym:
Target: Others
PW0464
T36946
Synonym: PW0464
Target:
AY 254
T41189
Synonym:
Target:
MM 07
TP2000
Synonym:
Target:
SAR247799
T38716
Synonym: SAR247799,S1P1 agonist 3
Target:
DL 175
T37907
Synonym:
Target:
NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
T76224
Synonym:
Target:
α-Conotoxin MrIC
T80471
Synonym:
Target:
ATI-2341 TFA (1337878-62-2 free base)
TP1354
Synonym: ATI-2341 TFA
Target:
UCSF678
T60597
Synonym:
Target:
UNC9994 hydrochloride
T62853
Synonym:
Target:
HCAR2 agonist 1
T82233
Synonym:
Target:
ATI-2341 TFA
T75721
Synonym:
Target:
Bilaid C
T37199
Synonym:
Target:

Recombinant Proteins

カタログ番号 製品名 Species Expression System
TMPJ-00837 LAMP1 Protein, Mouse, Recombinant (His) Mouse HEK293 Cells
Lysosomal associated membrane protein 1 (LAMP1) is an approximately 120 kDa transmembrane glycoprotein that is a major protein component of lysosomal membranes. Mature mouse LAMP1 consists of a 346 amino acid (aa) intral...