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TAK-875

规格或纯度: ≥98%

CAS编号: 1000413-72-8
分子式: C₂₉H₃₂O₇S
分子量: 524.64
PubChem编号: 24857286

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货号 (SKU)	包装规格	是否现货
T127963-5mg	5mg	现货
T127963-10mg	10mg	现货
T127963-25mg	25mg	现货
T127963-50mg	50mg	现货
T127963-100mg	100mg	现货

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FFA1 receptor Agonist

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基本描述

规格或纯度	≥98%
英文名称	TAK-875
别名	TAK 875;TAK875
英文别名	Fasiglifam;TAK 875;TAK875;(3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid;2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]a
生化机理	TAK-876 is a selective G protein-coupled receptor 40 (GPR40) agonist that has been developed to improve the secretion of insulin in a glucose-dependent manner.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Fasiglifam (TAK-875)是一种选择性GPR40激动剂，在表达人GPR40的CHO细胞系中EC50为14 nM，比油酸有效400倍。 TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM. A selective G protein-coupled receptor 40 (GPR40) agonist.

名称和标识符

IUPAC Name	2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid
INCHI	InChI=1S/C29H32O7S/c1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24/h4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31)/t23-/m1/s1
InChi Key	BZCALJIHZVNMGJ-HSZRJFAPSA-N
Canonical SMILES	CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C
分子式	C₂₉H₃₂O₇S
PubChem CID	24857286
分子量	524.64

数据库链接

PubChem CID	24857286
CAS Registry No.	1000413-72-8
ChEMBL Ligand	CHEMBL1829174
RCSB PDB Ligand	2YB
GPCRdb Ligand	fasiglifam

化学和物理性质

溶解性	DMSO ≥100mg/mL Water <1.2mg/mL Ethanol ≥10mg/mL
熔点	123-127°C

靶标

Target ID

225

名称

FFA1 receptor

缩写名

SHP2

家族

Free fatty acid receptors

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Rat	7	300	1q21	Ffar1	free fatty acid receptor 1
Human	7	300	19q13.12	FFAR1	free fatty acid receptor 1
Mouse	7	300	7 B1	Ffar1	free fatty acid receptor 1

RefSeq Protein

NP_695216 (Rn) , NP_005294 (Hs) , NP_918946 (Mm)

UniProtKB

Q8K3T4 (Rn) , O14842 (Hs) , Q76JU9 (Mm)

OMIM

603820 (Hs)

RefSeq Nucleotide

NM_005303 (Hs) , NM_153304 (Rn) , NM_194057 (Mm)

Entrez Gene

2864 (Hs) , 266607 (Rn) , 233081 (Mm)

Ensembl Gene

ENSG00000126266 (Hs) , ENSMUSG00000044453 (Mm) , ENSRNOG00000024009 (Rn)

Protein GI

23463291 (Rn) , 4885327 (Hs) , 110835701 (Mm)

GPCRdb

ffar1_human (Hs) , ffar1_mouse (Mm) , ffar1_rat (Rn)

UniProtKB ID/Entry name

FFAR1_HUMAN (Hs) , FFAR1_MOUSE (Mm) , FFAR1_RAT (Rn)

DrugBank Target

O14842 (Hs)

ChEMBL Target

CHEMBL5411 (Mm) , CHEMBL4422 (Hs) , CHEMBL1795180 (Rn)

关联配体

Ligand ID	6484
名称	fasiglifam
别名	TAK875
类别	Synthetic organic
学名	2-[(3S)-6-({3-[4-(3-methanesulfonylpropoxy)-2,6-dimethylphenyl]phenyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	Fasiglifam is a positive allosteric modulator/partial agonist of the free fatty acid receptor 1 (FFA1, a.k.a. GPR40) . In the presence of endogenous free fatty acids (FFAs) fasiglifam enhances insulin secretion, by binding to an allosteric site distinct from the orthosteric FFA binding site. On its own, it elicits a low level of insulin secretion. These findings indicate that fasiglifam acts cooperatively with FFAs to promote insulin secretion.

参考文献

1. Itoh Y, Kawamata Y, Harada M, Kobayashi M, Fujii R, Fukusumi S, Ogi K, Hosoya M, Tanaka Y, Uejima H et al.. (2003) Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.. Nature, 422 (6928): (173-6). [PMID:12629551]
2. Yabuki C, Komatsu H, Tsujihata Y, Maeda R, Ito R, Matsuda-Nagasumi K, Sakuma K, Miyawaki K, Kikuchi N, Takeuchi K et al.. (2013) A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.. PLoS ONE, 8 (10): (e76280). [PMID:24130766]