WS 3

WS 3 is an agonist of TRPM8 receptor with EC50 value of 3.7 μM [1].

Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca2+- and Na+-permeable ion channel and is activated by cooling agents and cold temperatures. TRPM8 belongs to TRP family and is expressed in sensory neurons.

WS 3 is an agonist of TRPM8 receptor and a cooling agent. In HEK293 cells expressed recombinant mouse TRPM8, WS 3 (30 μM) increased [Ca2+]i. WS 3 exhibited potency with EC50 value of 3.7 μM and induced 86% efficacy of the maximal response to icilin, the most potent agonist [1]. In HEK cells stably expressing either hTRPM8 or hTRPA1, WS 3 activated hTRPM8 and hTRPA1 with EC50 values of 2.2 and 120.6 μM, respectively. WS 3 was efficacious in eliciting cooling sensation [2].

References:
[1].  Behrendt HJ, Germann T, Gillen C, et al. Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol, 2004, 141(4): 737-745.
[2].  Klein AH, Iodi Carstens M, McCluskey TS, et al. Novel menthol-derived cooling compounds activate primary and second-order trigeminal sensory neurons and modulate lingual thermosensitivity. Chem Senses, 2011, 36(7): 649-658.

Abnormal photocurrent response and enhanced photocatalytic activity induced by charge transfer between WS(2) nanosheets and WO(3) nanoparticles.[Pubmed:24227745]

Chemphyschem. 2013 Dec 16;14(18):4069-73.

Sun trap: Pure WS2 nanosheets are prepared that exhibit excellent photosensitive properties. After functionalization with WO3 nanoparticles, abnormal photocurrent responses, enhanced photocatalytic activity, and induced photoluminescence is observed.

WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: a novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity.[Pubmed:19828876]

J Pharmacol Exp Ther. 2010 Jan;332(1):190-201.

The preclinical characterization of WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one] is described. In vitro binding and functional studies revealed highest affinity to the D(2) receptor (D(2L) K(i), 4.0 nM) and serotonin transporter (K(i), 7.1 nM), potent D(2) partial agonist activity (EC(50), 0.38 nM; E(max), 30%), and complete block of the serotonin transporter (IC(50), 56.4 nM). Consistent with this in vitro profile, WS-50030 (10 mg/kg/day, 21 days) significantly increased extracellular 5-HT in the rat medial prefrontal cortex, short-term WS-50030 treatment blocked apomorphine-induced climbing (ID(50), 0.51 mg/kg) in a dose range that produced minimal catalepsy in mice and induced low levels of contralateral rotation in rats with unilateral substantia nigra 6-hydroxydopamine lesions (10 mg/kg i.p.), a behavioral profile similar to that of the D(2) partial agonist aripiprazole. In a rat model predictive of antipsychotic-like activity, WS-50030 and aripiprazole reduced conditioned avoidance responding by 42 and 55% at 10 mg/kg, respectively. Despite aripiprazole's reported lack of effect on serotonin transporters, long-term treatment with aripiprazole or WS-50030 reversed olfactory bulbectomy-induced hyperactivity at doses that did not reduce activity in sham-operated rats, indicating antidepressant-like activity for both compounds. Despite possessing serotonin reuptake inhibitory activity in addition to D(2) receptor partial agonism, WS-50030 displays activity in preclinical models predictive of antipsychotic- and antidepressant efficacy similar to aripiprazole, suggesting potential efficacy of WS-50030 versus positive and negative symptoms of schizophrenia, comorbid mood symptoms, bipolar disorder, major depressive disorder, and treatment-resistant depression. Furthermore, WS-50030 provides a tool to further explore how combining these mechanisms might differentiate from other antipsychotics or antidepressants.

Stepwise addition of CuNCS onto [Et(4)N][Tp*WS(3)]: design, syntheses, structures and third-order nonlinear optical properties.[Pubmed:19381405]

Dalton Trans. 2009 May 14;(18):3425-33.

Stepwise reactions of [Et(4)N][Tp*WS(3)] () (Tp* = hydridotris(3,5-dimethylpyrazol-1-yl)borate) with 1-4 equiv. of CuNCS (and Et(4)NBr in the case of three equiv. of CuNCS) afforded the [1 + 1] to [1 + 4] addition products [Et(4)N][Tp*WS(mu-S)(2)(CuNCS)].0.5CH(2)Cl(2) (.0.5CH(2)Cl(2)), [Et(4)N][Tp*W(mu(3)-S)(mu-S)(2)(CuNCS)(2)].ClCH(2)CH(2)Cl (.ClCH(2)CH(2)Cl), [Et(4)N](2)[Tp*W(mu(3)-S)(3)(CuNCS)(3)(mu(3)-Br)].1.5aniline (.1.5aniline), and {[Et(4)N][Tp*W(mu(3)-S)(3)(Cu-mu-SCN)(3)(Cu-mu(3)-NCS)]}(n) (). Compounds were characterized by elemental analysis, IR spectra, UV-vis spectra, (1)H NMR, and single-crystal X-ray crystallography. The cluster anion of contains a [WS(2)Cu] core formed by addition of one CuNCS group onto the [Tp*WS(3)] species. The cluster anion of has a butterfly-shaped [WS(3)Cu(2)] core constructed by addition of two CuNCS groups onto the [Tp*WS(3)] species. The cluster dianion of consists of a cubane-like [Tp*WS(3)Cu(3)(mu(3)-Br)] core assembled by addition of three CuNCS groups onto the [Tp*WS(3)] species followed by filling a mu(3)-Br into the void of the incomplete cubane-like [Tp*WS(3)(CuNCS)(3)] fragment. has a 2D cluster-supported layer network in which each [Tp*WS(3)Cu(3)] core acting as a pyramidal 3-connecting node interconnects with the [Cu(NCS)(4)] units through thiocyanate bridges. In addition, the third-order nonlinear optical (NLO) performances of in DMF were also investigated by Z-scan techniques.

β cell proliferation agonist WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).

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