Grouped product items

SKU

Size

Availability

Price

Qty

T127963-5mg

5mg

In stock

$129.90

T127963-10mg

10mg

In stock

$195.90

T127963-25mg

25mg

In stock

$441.90

T127963-50mg

50mg

In stock

$587.90

T127963-100mg

100mg

Available within 4-8 weeks(?)

$966.90

Basic Description

Synonyms	Fasiglifam\|TAK-875\|1000413-72-8\|TAK875\|TAK 875\|(S)-2-(6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid\|Tak-875 anhydrous\|GLP1W4JXAH\|TAK-875(Fasiglifam)\|3-Benzofuranacetic acid, 6-[[2',6
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	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.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	AGONIST, POSITIVE ALLOSTERIC MODULATOR
Mechanism of action	Free fatty acid receptor 1 positive allosteric modulator
Product Description	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.

Product Properties

ALogP	4.7

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Discover Target: CYP2D6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

Discover Target: CX3CR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR35 Tchem G-protein coupled receptor 35 0 Activities

Discover Target: GPR35

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Discover Target: CYP2C9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

Discover Target: FFAR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FFAR1 Tchem Free fatty acid receptor 1 31 Activities

Discover Target: FFAR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

Discover Target: FPR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Discover Target: CSNK1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 0 Activities

Discover Target: SLCO1B1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 0 Activities

Discover Target: SLCO1B3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

Discover Target: S1PR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Discover Target: TRIM24

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCC2 Tchem Canalicular multispecific organic anion transporter 1 0 Activities

Discover Target: ABCC2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

Discover Target: ADRB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

APLNR Tchem Apelin receptor 0 Activities

Discover Target: APLNR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Discover Target: ADRA2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

Discover Target: GPR119

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

Discover Target: GLP1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARA Tclin Peroxisome proliferator-activated receptor alpha 0 Activities

Discover Target: PPARA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARD Tchem Peroxisome proliferator-activated receptor delta 0 Activities

Discover Target: PPARD

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC10A1 Tclin Sodium/bile acid cotransporter 0 Activities

Discover Target: SLC10A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARG Tclin Peroxisome proliferator-activated receptor gamma 0 Activities

Discover Target: PPARG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

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
Isomeric SMILES	CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)[C@@H](CO4)CC(=O)O)C)OCCCS(=O)(=O)C
PubChem CID	24857286
Molecular Weight	524.64

Database links

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

Certificates

Certificate of Analysis(COA)

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5 results found

Lot Number	Certificate Type	Date	Item
A2219438	Certificate of Analysis	Nov 10, 2023	T127963
A2219440	Certificate of Analysis	Nov 10, 2023	T127963
A2219499	Certificate of Analysis	Nov 10, 2023	T127963
A2219697	Certificate of Analysis	Nov 10, 2023	T127963
A2219699	Certificate of Analysis	Nov 10, 2023	T127963

Chemical and Physical Properties

Solubility	DMSO ≥100mg/mL Water <1.2mg/mL Ethanol ≥10mg/mL
Melt Point(°C)	123-127°C

References

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]

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TAK-875 - ≥98%, high purity , Free fatty acid receptor 1 positive allosteric modulator, CAS No.1000413-72-8, Free fatty acid receptor 1 positive allosteric modulator

Basic Description

Product Properties

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

GPR35 Tchem G-protein coupled receptor 35 0 Activities

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

FFAR1 Tchem Free fatty acid receptor 1 31 Activities

HDAC6 Tclin Histone deacetylase 6 0 Activities

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 0 Activities

SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 0 Activities

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

ABCC2 Tchem Canalicular multispecific organic anion transporter 1 0 Activities

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

BRPF1 Tchem Peregrin 0 Activities

AURKA Tchem Aurora kinase A 0 Activities

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

APLNR Tchem Apelin receptor 0 Activities

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

PPARA Tclin Peroxisome proliferator-activated receptor alpha 0 Activities

PPARD Tchem Peroxisome proliferator-activated receptor delta 0 Activities

SLC10A1 Tclin Sodium/bile acid cotransporter 0 Activities

PPARG Tclin Peroxisome proliferator-activated receptor gamma 0 Activities

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

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References

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