cas 154902-51-9, BOC-L-3-BENZOTHIENYLALANINE

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154902-51-9

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INHIBITORS OF AKT ACTIVITY
Invented are novel pyridine compounds, the use of such compounds as inhibitors of PKB/AKT kinase activity and in the treatment of cancer and arthritis.
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Page/Page column 47; 117

(2010/02/14)

Studies of Neurokinin Antagonists. 4. Synthesis and Structure-Activity Relationships of Novel Dipeptide Substance P Antagonists: N2--L-prolyl>-N-methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and Its Related Compounds
As an extension of our studies on discovering a novel substance P (SP) antagonist, we modified the previously reported dipeptide, N2-2-(1H-indol-3-ylcarbonyl)-L-lysyl>-N-methyl-N-(phenylmethyl)-L-phenylalaninamide (2b).The lysine part in 2b was first optimized to a (2S,4R)-hydroxyproline derivative (3h), which is 2-fold more potent than 2b in SP binding assay using guinea pig lung membranes.Next we modified the 1H-indol-3-ylcarbonyl part in 3h.Introduction of a methyl group at the indole nitrogen enhanced the oral activity, while retaining the binding activity.Finally, we modified the phenylalanine part to culminate in the most potent compound 7k (FK888), which is a potent SP antagonist with NK1 selectivity as well as oral activity.
Hagiwara, Daijiro,Miyake, Hiroshi,Igari, Norihiro,Karino, Masako,Maeda, Yasue,et al.
p. 2090 - 2099
(2007/10/02)

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N²-Boc-N-methyl-N-(phenylmethyl)-3-(3-benzothienyl)-L-alaninamide

Chemical Properties

Boiling Point: 514.1 °C at 760 mmHg

Flash Point:264.7 °C

Density: 1.274 g/cm³

Storage Temp.:-15°C

Vapor Pressure: 2.56E-09mmHg at 25°C

Refractive Index: 1.53

PKA: 3.85±0.10(Predicted)

BRN: 7081201

PSA: 103.87000

LogP: 3.81260

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154902-51-9

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Chemical Properties

Boiling Point: 514.1 °C at 760 mmHg

Flash Point:264.7 °C

Density: 1.274 g/cm3

Storage Temp.:-15°C

Vapor Pressure: 2.56E-09mmHg at 25°C

Refractive Index: 1.53

PKA: 3.85±0.10(Predicted)

BRN: 7081201

PSA: 103.87000

LogP: 3.81260

Global suppliers and manufacturers of 154902-51-9total 35 suppliers on LookChem

Density: 1.274 g/cm³