1000413-72-8 Usage
Description
TAK-875 is a selective free fatty acid receptor 1 (FFAR1; GPR40) agonist with a high affinity (EC50 = 26 nM) for its target receptor. It is a novel compound that does not exhibit activity on related FFARs, such as FFAR2 (GPR43) or FFAR3 (GPR41). TAK-875 is significant due to its potential role in regulating diabetes, obesity, and other metabolic disorders by targeting the FFAR1 signaling pathway, which is linked to the amplification of glucose-stimulated insulin secretion.
Uses
Used in Pharmaceutical Industry:
TAK-875 is used as a selective FFAR1 (GPR40) agonist for the development of novel oral medications aimed at improving insulin secretion in a glucose-dependent manner. This application is particularly relevant for the treatment and management of diabetes, as it has the potential to enhance blood sugar control with a low risk of hypoglycemia.
Used in Metabolic Disorder Research:
TAK-875 is used as a research tool to investigate the role of FFAR1 (GPR40) in metabolic disorders such as diabetes and obesity. By selectively activating this receptor, researchers can gain insights into the underlying mechanisms and pathways involved in these conditions, potentially leading to the development of new therapeutic strategies.
Used in Drug Development:
TAK-875 serves as a starting point for the development of new drugs targeting the FFAR1 (GPR40) receptor. Its selectivity and potency make it an attractive candidate for further optimization and modification to improve its pharmacological properties, such as bioavailability, stability, and efficacy. This could lead to the creation of more effective treatments for metabolic disorders and other related conditions.
in vitro
tak-875 exhibited potent agonist activity and high binding affinity to the human receptor. in addition, tak-875 showed excellent agonist potency selectivity for gpr40 receptor over other members of the ffa receptor family (for which ec50>10 μm) [1].
in vivo
tak-875 showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female wistar fatty rats with impaired glucose tolerance [2].
references
[1] negoro n, sasaki s, mikami s, ito m, suzuki m, tsujihata y, ito r, harada a, takeuchi k, suzuki n, miyazaki j, santou t, odani t, kanzaki n, funami m, tanaka t1, kogame a, matsunaga s, yasuma t, momose y. discovery of tak-875: a potent, selective, and orally bioavailable gpr40 agonist. acs med chem lett. 2010 jun 18;1(6):290-4. [2] leifke e, naik h, wu j, viswanathan p, demanno d, kipnes m, vakilynejad m. a multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel gpr40 agonist, tak-875, in subjects with type 2 diabetes. clin pharmacol ther. 2012 jul;92(1):29-39.
Check Digit Verification of cas no
The CAS Registry Mumber 1000413-72-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,0,4,1 and 3 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1000413-72:
(9*1)+(8*0)+(7*0)+(6*0)+(5*4)+(4*1)+(3*3)+(2*7)+(1*2)=58
58 % 10 = 8
So 1000413-72-8 is a valid CAS Registry Number.
1000413-72-8Relevant articles and documents
A 2 - (6-hydroxy -2,3-dihydrobenzo-furan-3-yl) acetonitrile TAK-875 compound preparation compound and method
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, (2016/12/01)
The present invention particularly relates to a chiral compound 2-(6-hydroxy-2,3-dihydro benzofuran-3-yl)acetonitrile and a preparation method thereof, and a method for preparing a TAK-875 drug by adopting the compound as an intermediate. Compared with the TAK-875 synthesis method reported in the literature, the method for preparing the TAK-875 by adopting the chiral compound 2-(6-hydroxy-2,3-dihydro benzofuran-3-yl)acetonitrile in the present invention has the following advantages that: the single maximum impurity, the content, the yield, the optical purity and other characteristics of the obtained TAK-875 in the present invention are superior to the TAK-875 obtained through the method in the literature, and the method is suitable for industrial mass production.
FUSED CYCLIC COMPOUNDS
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Page/Page column 115-116, (2008/06/13)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
