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WS3

Names

[ CAS No. ]:
1421227-52-2

[ Name ]:
WS3

[Synonym ]:
N-(6-{4-[({4-[(4-Methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}carbamoyl)amino]phenoxy}-4-pyrimidinyl)cyclopropanecarboxamide
Cyclopropanecarboxamide, N-[6-[4-[[[[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-4-pyrimidinyl]-
WS3

Biological Activity

[Description]:

WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).EC50 value: 28 nM [1]Target: β cell proliferation agonistProtocol(Only for Reference) [1]In vivo efficacy studies in RIP-DTA mice:RIP-DTA mice were purchased from Jackson Laboratories and all aspects of their treatment were outlined in a protocol approved by an internal animal care and use committee (IACUC). Mice were housed as 3-5 mice per cage and fed standard chow and water. During disease induction, doxycycline was added to the drinking water at a concentration of 2 mg/mL. Animals were injected intraperitoneally with saline-formulated WS6 at 5 mg/kg once every other day (for efficacy study). Blood glucose was monitored every third day. Mice were sacrificed at the end of week 1 and pancreas was fixed in formalin, sectioned, and stained for Ki67 and insulin. At the end of week 6, wet pancreas weight was recorded, and fixed pancreata were sectioned and stained for insulin; total insulin area and wet weight were used to calculate beta cell mass. For pharmacokinetic studies, WS6 was formulated at 50 mg/kg and given as single intraperitoneal dose, followed by serum collection and analysis of compound concentration in serum to determine CMAX and half-life (T1/2).

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[References]

[1]. Shen W, et al. Small-molecule inducer of β cell proliferation identified by high-throughput screening. J Am Chem Soc. 2013 Feb 6;135(5):1669-72.


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Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
632.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H30F3N7O3

[ Molecular Weight ]:
569.578

[ Flash Point ]:
336.6±31.5 °C

[ Exact Mass ]:
569.236206

[ PSA ]:
111.72000

[ LogP ]:
4.37

[ Appearance of Characters ]:
white to beige

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.657

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: soluble10mg/mL, clear

Safety Information

[ RIDADR ]:
NONH for all modes of transport


Related Compounds

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