INT-777 (S-EMCA) [CAS 1199796-29-6] - ChemeGen-活性小分子-抑制剂-激动剂

信号通路

Anti-infection
Arenavirus
Bacterial
CMV
Enterovirus
Filovirus
Fungal
HBV
HCV
HIV
HSV
Influenza Virus
Parasite
Reverse Transcriptase
RSV
SARS-CoV
Virus Protease
Antibody-drug Conjugate/ADC Related
ADC Cytotoxin
ADC Linker
Drug-Linker Conjugates for ADC
PROTAC-linker Conjugate for PAC
Apoptosis
Apoptosis
FKBP
Bcl-2 Family
c-Myc
Caspase
DAPK
Ferroptosis
IAP
MDM-2/p53
PKD
RIP kinase
Survivin
Thymidylate Synthase
TNF Receptor
Autophagy
Autophagy
LRRK2
Mitophagy
ULK
Cell Cycle/DNA Damage
Antifolate
APC
ATM/ATR
Aurora Kinase
Casein Kinase
CDK
Checkpoint Kinase (Chk)
CRISPR/Cas9
Deubiquitinase
DNA Alkylator/Crosslinker
DNA-PK
DNA/RNA Synthesis
Eukaryotic Initiation Factor (eIF)
G-quadruplex
Haspin Kinase
HDAC
HSP
IRE1
Kinesin
LIM Kinase (LIMK)
Microtubule/Tubulin
Mps1
Nucleoside Antimetabolite/Analog
p97
PAK
PARP
PERK
Polo-like Kinase (PLK)
PPAR
RAD51
ROCK
Sirtuin
SRPK
Telomerase
TOPK
Topoisomerase
Wee1
Cytoskeleton
Arp2/3 Complex
Dynamin
Gap Junction Protein
Integrin
Kinesin
Microtubule/Tubulin
Mps1
Myosin
PAK
Epigenetics
AMPK
Aurora Kinase
DNA Methyltransferase
Epigenetic Reader Domain
HDAC
Histone Acetyltransferase
Histone Demethylase
Histone Methyltransferase
JAK
MicroRNA
PARP
PKC
Protein Arginine Deiminase
TAM Receptor
Sirtuin
GPCR/G Protein
5-HT Receptor
Adenosine Receptor
Adenylate Cyclase
Adiponectin Receptor
Adrenergic Receptor
Angiotensin Receptor
Bombesin Receptor
Bradykinin Receptor
Cannabinoid Receptor
CaSR
CCR
CGRP Receptor
Cholecystokinin Receptor
CRFR
CXCR
Dopamine Receptor
EBI2/GPR183
Endothelin Receptor
GHSR
Glucagon Receptor
Glucocorticoid Receptor
GNRH Receptor
GPCR19
GPR109A
GPR119
GPR120
GPR139
GPR40
GPR55
GPR84
Guanylate Cyclase
Histamine Receptor
Imidazoline Receptor
Leukotriene Receptor
LPL Receptor
mAChR
MCHR1 (GPR24)
Melanocortin Receptor
Melatonin Receptor
mGluR
Motilin Receptor
Neurokinin Receptor
Neuropeptide Y Receptor
Neurotensin Receptor
Opioid Receptor
Orexin Receptor (OX Receptor)
Oxytocin Receptor
P2Y Receptor
Prostaglandin Receptor
Protease-Activated Receptor (PAR)
Ras
RGS Protein
Sigma Receptor
Somatostatin Receptor
TSH Receptor
Urotensin Receptor
Vasopressin Receptor
Immunology/Inflammation
Arginase
Aryl Hydrocarbon Receptor
CCR
Complement System
COX
CXCR
FLAP
Histamine Receptor
IFNAR
Interleukin Related
IRAK
MyD88
NO Synthase
NOD-like Receptor (NLR)
PD-1/PD-L1
PGE synthase
Salt-inducible Kinase (SIK)
SPHK
STING
Thrombopoietin Receptor
Toll-like Receptor (TLR)
CD73
Reactive Oxygen Species
Galectin
JAK/STAT Signaling
EGFR
JAK
Pim
STAT
MAPK/ERK Pathway
ERK
JNK
KLF
MAP3K
MAP4K
MAPKAPK2 (MK2)
MEK
Mixed Lineage Kinase
MNK
p38 MAPK
Raf
Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel
ATP Synthase
BCRP
Calcium Channel
CFTR
Chloride Channel
CRAC Channel
CRM1
EAAT2
GABA Receptor
GlyT
HCN Channel
iGluR
Monoamine Transporter
Monocarboxylate Transporter
Na+/Ca2+ Exchanger
Na+/HCO3- Cotransporter
Na+/K+ ATPase
nAChR
NKCC
P-glycoprotein
P2X Receptor
Potassium Channel
Proton Pump
SGLT
Sodium Channel
TRP Channel
URAT1
Metabolic Enzyme/Protease
15-PGDH
5 alpha Reductase
5-Lipoxygenase
Acetyl-CoA Carboxylase
Acyltransferase
Adenosine Deaminase
Adenosine Kinase
Aldehyde Dehydrogenase (ALDH)
Aldose Reductase
Aminoacyl-tRNA Synthetase
Aminopeptidase
Angiotensin-converting Enzyme (ACE)
Arginase
ATGL
ATP Citrate Lyase
Carbonic Anhydrase
Carboxypeptidase
Cathepsin
CETP
COMT
Cytochrome P450
Dipeptidyl Peptidase
Dopamine β-hydroxylase
Drug Metabolite
E1/E2/E3 Enzyme
Elastase
Endogenous Metabolite
Enolase
FAAH
FABP
Factor Xa
Farnesyl Transferase
Fatty Acid Synthase (FAS)
FXR
Glucokinase
GSNOR
Gutathione S-transferase
HCV Protease
Hexokinase
HIF/HIF Prolyl-Hydroxylase
HIV Integrase
HIV Protease
HMG-CoA Reductase (HMGCR)
HSP
Indoleamine 2,3-Dioxygenase (IDO)
Isocitrate Dehydrogenase (IDH)
Lactate Dehydrogenase
LXR
MAGL
Mineralocorticoid Receptor
Mitochondrial Metabolism
MMP
NADPH Oxidase
Nampt
NEDD8-activating Enzyme
Neprilysin
PAI-1
PDHK
PGC-1α
Phosphatase
Phosphodiesterase (PDE)
Phospholipase
Procollagen C Proteinase
Proteasome
Pyruvate Kinase
RAR/RXR
Renin
ROR
Ser/Thr Protease
SGK
Stearoyl-CoA Desaturase (SCD)
Thrombin
Tryptophan Hydroxylase
Tyrosinase
Xanthine Oxidase
Glutaminase
Glutathione Peroxidase
Neuronal Signaling
5-HT Receptor
AChE
Adenosine Kinase
Amyloid-β
Beta-secretase
CaMK
CGRP Receptor
COMT
Dopamine Receptor
Dopamine Transporter
FAAH
GABA Receptor
GlyT
iGluR
Imidazoline Receptor
mAChR
Melanocortin Receptor
Melatonin Receptor
Monoamine Oxidase
nAChR
Neurokinin Receptor
Opioid Receptor
Serotonin Transporter
γ-secretase
NF-κB
IKK
Keap1-Nrf2
MALT1
NF-κB
PI3K/Akt/mTOR
Akt
AMPK
ATM/ATR
DNA-PK
GSK-3
MELK
mTOR
PDK-1
PI3K
PI4K
PIKfyve
PTEN
PROTAC
E3 Ligase Ligand-Linker Conjugate
Ligand for E3 Ligase
PROTAC
PROTAC Linker
PROTAC-linker Conjugate for PAC
Ligand for Target Protein for PROTAC
SNIPER
Target Protein Ligand-Linker Conjugate
Protein Tyrosine Kinase/RTK
Ack1
ALK
Bcr-Abl
BMX Kinase
Btk
c-Fms
c-Kit
c-Met/HGFR
Discoidin Domain Receptor
DYRK
EGFR
Ephrin Receptor
FAK
FGFR
FLT3
IGF-1R
Insulin Receptor
IRAK
Itk
PDGFR
PKA
Pyk2
ROS
Src
Syk
TAM Receptor
Trk Receptor
VEGFR
RET
Stem Cell/Wnt
Casein Kinase
ERK
Gli
GSK-3
Hedgehog
Hippo (MST)
JAK
Notch
Oct3/4
PKA
Porcupine
ROCK
sFRP-1
Smo
STAT
TGF-beta/Smad
Wnt
YAP
β-catenin
γ-secretase
TGF-beta/Smad
PKC
ROCK
TGF-beta/Smad
TGF-β Receptor
Vitamin D Related
VD/VDR
Others
Androgen Receptor
Aromatase
Estrogen Receptor/ERR
Progesterone Receptor
Thyroid Hormone Receptor
Others
Inhibitory Antibodies
Cytokines
ADC
Epigenetic Reader Dom

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INT-777 (S-EMCA) [CAS 1199796-29-6]

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产品详情

Cat. No.：	C100577	CAS：	1199796-29-6
Formula：	C27H46O5	MWt：	450.65
Purity：	≥98%	Solubility：	DMSO
Storage：	Powder -20°C 3 years; 4°C 2 years In solvent -80°C 6 months;-20°C 1 month	Research Area：	Endocrinology
Target：	EC50: 0.82 μM (TGR5)[1]	Description：	INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM.

[1]. Pellicciari R, et al. Discovery of 6alphaethyl23(S)methylcholic acid (SEMCA, INT777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem. 2009 Dec 24;52(24):7958-61.

[2]. Thomas C, et al. TGR5mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009 Sep;10(3):167-77.

[3]. Duboc H, et al.Reduction of epithelial secretion in male rat distal colonic mucosa by bile acid receptor TGR5 agonist, INT-777: role of submucosal neurons. Neurogastroenterol Motil. 2016 Jun 3. doi: 10.1111/nmo.

[4]. Pellicciari R, et al. Discovery of 6alphaethyl23(S)methylcholic acid (SEMCA, INT777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. Format: AbstractSend to J Med Chem. 2009 Dec 24;52(24):7958-61.

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