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TUG-770

CAS编号: 1402601-82-4
分子式: C₁₉H₁₄FNO₂
分子量: 307.32
PubChem编号: 66553168

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货号 (SKU)	包装规格	是否现货
T126560-1mg	1mg	期货
T126560-5mg	5mg	期货
T126560-10mg	10mg	期货
T126560-25mg	25mg	期货
T126560-50mg	50mg	期货
T126560-100mg	100mg	期货

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FFA1 receptor Agonist

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基本描述

英文名称	TUG-770
生化机理	Description: IC50 Value: 6nM (hFFA1) [1] Tμg-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. in vitro: Tμg-770 (Compound 22) displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). Tμg-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drμg-drμg interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay [1]. in vivo: Examination of Tμg-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of Tμg-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of Tμg-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min [1]. Clinical trial: N/A
储存温度	-20°C储存
运输条件	超低温冰袋运输

名称和标识符

IUPAC Name	3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
INCHI	InChI=1S/C19H14FNO2/c20-18-13-14(6-8-17(18)9-10-19(22)23)5-7-15-3-1-2-4-16(15)11-12-21/h1-4,6,8,13H,9-11H2,(H,22,23)
InChi Key	KIZUBVPJNPVIIN-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F
分子式	C₁₉H₁₄FNO₂
PubChem CID	66553168
分子量	307.32

数据库链接

PubChem CID	66553168
ChEMBL Ligand	CHEMBL2386353
CAS Registry No.	1402601-82-4
GPCRdb Ligand	TUG-770

化学和物理性质

溶解性	25°C: DMSO

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	6483
名称	TUG-770
别名	TUG770
类别	Synthetic organic
学名	3-(4-{2-[2-(cyanomethyl)phenyl]ethynyl}-2-fluorophenyl)propanoic 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	Sulfadimidine (sulfamethazine) is a sulfonamide antibacterial compound. This class of compounds are competitive inhibitors of bacterial dihydropteroate synthase (DHPS), an enzyme in the pathway which generates the folic acid that is essential for bacterial growth.