Category: 317318-97-1

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.317318-97-1, Name is 5-(Chloromethyl)-4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole, molecular formula is C12H9ClF3NS. In a Patent£¬once mentioned of 317318-97-1, HPLC of Formula: C12H9ClF3NS

The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPARdelta), and also provides processes for compounds of formula (VI), (VII), (VIII) and (IX), intermediate compounds for preparation of the above compounds of formula (XI).

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 317318-97-1 is helpful to your research., HPLC of Formula: C12H9ClF3NS

Reference£º
Thiazole | C3H5995NS – PubChem,
Thiazole | chemical compound | Britannica

Related Products of 317318-97-1, An article , which mentions 317318-97-1, molecular formula is C12H9ClF3NS. The compound – 5-(Chloromethyl)-4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole played an important role in people’s production and life.

The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancement of glucose-stimulated insulin secretion. Takeda’s compound 1 has robustly in vitro activity for FFA1, but it has been suffered from poor pharmacokinetic (PK) profiles because the phenylpropanoic acid is vulnerable to beta-oxidation. To identify orally available agonists, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the alpha-position of phenylpropionic acid. Interestingly, the differences of physicochemical properties between hydrogen and deuterium are quite small, but there are many differences in the structure-activity relationship between phenylpropionic acid series and present deuterated series. Further optimizations of deuterated series led to the discovery of compound 18, which exhibited a superior balance in terms of in vitro activity, lipophilicity, and solubility. Better still, compound 18 revealed a lower clearance (CL = 0.44 L/h/kg), higher maximum concentration (Cmax = 7584.27 mug/L), and longer half-life (T1/2 = 4.16 h), resulting in a >23-fold exposure than compound 1. In subsequent in vivo pharmacodynamic studies, compound 18 showed a robustly glucose-lowering effect in rodent without the risk of hypoglycemia.

The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancement of glucose-stimulated insulin secretion. Takeda’s compound 1 has robustly in vitro activity for FFA1, but it has been suffered from poor pharmacokinetic (PK) profiles because the phenylpropanoic acid is vulnerable to beta-oxidation. To identify orally available agonists, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the alpha-position of phenylpropionic acid. Interestingly, the differences of physicochemical properties between hydrogen and deuterium are quite small, but there are many differences in the structure-activity relationship between phenylpropionic acid series and present deuterated series. Further optimizations of deuterated series led to the discovery of compound 18, which exhibited a superior balance in terms of in vitro activity, lipophilicity, and solubility. Better still, compound 18 revealed a lower clearance (CL = 0.44 L/h/kg), higher maximum concentration (Cmax = 7584.27 mug/L), and longer half-life (T1/2 = 4.16 h), resulting in a >23-fold exposure than compound 1. In subsequent in vivo pharmacodynamic studies, compound 18 showed a robustly glucose-lowering effect in rodent without the risk of hypoglycemia.

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Reference£º
Thiazole | C3H6002NS – PubChem,
Thiazole | chemical compound | Britannica

Electric Literature of 317318-97-1, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 317318-97-1, C12H9ClF3NS. A document type is Article, introducing its new discovery.

A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARdelta selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a, 12c, 17a and 18a showed PPAR-pan agonists activities and among these four compounds tested, 12a emerged as highly potent and efficacious compound, while 17a exhibited moderate and balanced PPAR-pan agonistic activity. In vivo, selected test compounds 12a and 17a exhibited significant anti-hyperglycemic and anti-hyperlipidemic activities in relevant animal models. These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists.

A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARdelta selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a, 12c, 17a and 18a showed PPAR-pan agonists activities and among these four compounds tested, 12a emerged as highly potent and efficacious compound, while 17a exhibited moderate and balanced PPAR-pan agonistic activity. In vivo, selected test compounds 12a and 17a exhibited significant anti-hyperglycemic and anti-hyperlipidemic activities in relevant animal models. These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists.

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Reference£º
Thiazole | C3H6014NS – PubChem,
Thiazole | chemical compound | Britannica

Synthetic Route of 317318-97-1. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 317318-97-1, Name is 5-(Chloromethyl)-4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole

We have discovered and demonstrated the in vitro and in vivo PPARdelta-selective activity of novel Y-shaped agonists. These compounds activated hPPARdelta with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARdelta agonists with 104-fold selectivity over the other two subtypes, namely, hPPARalpha and hPPARgamma. The PPARdelta ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.

We have discovered and demonstrated the in vitro and in vivo PPARdelta-selective activity of novel Y-shaped agonists. These compounds activated hPPARdelta with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARdelta agonists with 104-fold selectivity over the other two subtypes, namely, hPPARalpha and hPPARgamma. The PPARdelta ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.

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Reference£º
Thiazole | C3H5983NS – PubChem,
Thiazole | chemical compound | Britannica