SB 2283575-HT2C/2B antagonist/inverse agonist CAS# 181629-93-6 |
- Talnetant
Catalog No.:BCC1981
CAS No.:174636-32-9
- Talnetant hydrochloride
Catalog No.:BCC1982
CAS No.:204519-66-4
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 181629-93-6 | SDF | Download SDF |
PubChem ID | 443390 | Appearance | Powder |
Formula | C22H17F4N3O2 | M.Wt | 431.39 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO | ||
Chemical Name | N-(3-fluoro-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide | ||
SMILES | COC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC(=CC(=C3)C4=CN=CC=C4)F)C(F)(F)F | ||
Standard InChIKey | RRJLJKRFFRZRAF-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C22H17F4N3O2/c1-31-20-9-13-4-6-29(19(13)11-18(20)22(24,25)26)21(30)28-17-8-15(7-16(23)10-17)14-3-2-5-27-12-14/h2-3,5,7-12H,4,6H2,1H3,(H,28,30) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | 5-HT2C/2B receptor antagonist (pKi values are 7.0, 8.1 and 9.1 at 5-HT2A, 2B and 2C receptors respectively). Displays inverse agonism in a 5-HT-stimulated PI hydrolysis model of 5-HT2C receptor function. Orally active in vivo. |
SB 228357 Dilution Calculator
SB 228357 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.3181 mL | 11.5904 mL | 23.1809 mL | 46.3618 mL | 57.9522 mL |
5 mM | 0.4636 mL | 2.3181 mL | 4.6362 mL | 9.2724 mL | 11.5904 mL |
10 mM | 0.2318 mL | 1.159 mL | 2.3181 mL | 4.6362 mL | 5.7952 mL |
50 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 0.9272 mL | 1.159 mL |
100 mM | 0.0232 mL | 0.1159 mL | 0.2318 mL | 0.4636 mL | 0.5795 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- tert-Butyldimethylsilyl Chloride
Catalog No.:BCC2796
CAS No.:18162-48-6
- Isonemerosin
Catalog No.:BCN6550
CAS No.:181524-79-8
- PD 160170
Catalog No.:BCC7284
CAS No.:181468-88-2
- Colutehydroquinone
Catalog No.:BCN8239
CAS No.:181311-16-0
- Taxuspine W
Catalog No.:BCN6937
CAS No.:181309-92-2
- Ginsenoside F4
Catalog No.:BCN2881
CAS No.:181225-33-2
- DEL-22379
Catalog No.:BCC6521
CAS No.:181223-80-3
- Almotriptan Malate
Catalog No.:BCC5045
CAS No.:181183-52-8
- Co 102862
Catalog No.:BCC7439
CAS No.:181144-66-1
- 4,5-Dimethoxycanthin-6-one
Catalog No.:BCN1143
CAS No.:18110-87-7
- 5-Hydroxy-4-methoxycanthin-6-one
Catalog No.:BCN1142
CAS No.:18110-86-6
- Proflavine Hemisulfate
Catalog No.:BCC4707
CAS No.:1811-28-5
- Valdecoxib
Catalog No.:BCC4441
CAS No.:181695-72-7
- Interiotherins A
Catalog No.:BCN3093
CAS No.:181701-06-4
- Cyclopiazonic acid
Catalog No.:BCC6981
CAS No.:18172-33-3
- (-)-beta-Pinene
Catalog No.:BCN3857
CAS No.:18172-67-3
- 25-Anhydrocimigenol 3-O-beta-D-xyloside
Catalog No.:BCN3436
CAS No.:181765-11-7
- Crotonoside
Catalog No.:BCN6281
CAS No.:1818-71-9
- KC 12291 hydrochloride
Catalog No.:BCC7618
CAS No.:181936-98-1
- DLPC
Catalog No.:BCC7929
CAS No.:18194-25-7
- Sequirin C
Catalog No.:BCN4688
CAS No.:18194-29-1
- Fmoc-Dap-OH
Catalog No.:BCC3187
CAS No.:181954-34-7
- Naringenin-4',7-diacetate
Catalog No.:BCN1144
CAS No.:18196-13-9
- Angenomalin
Catalog No.:BCN8246
CAS No.:18199-64-9
The effect of Sb-surfactant on GaInP CuPtB type ordering: assessment through dark field TEM and aberration corrected HAADF imaging.[Pubmed:28367549]
Phys Chem Chem Phys. 2017 Apr 12;19(15):9806-9810.
We report on the effect of Sb on the microstructure of GaInP layers grown by metal organic vapor phase epitaxy (MOVPE). These layers exhibit a CuPtB single variant ordering due to the intentional misorientation of the substrate (Ge(001) substrates with 6 degrees misorientation towards the nearest [111] axis). The use of Sb as a surfactant during the GaInP growth does not modify the type of ordering, but it is found that the order parameter (eta) decreases with increasing Sb flux. Dark field microscopy reveals a variation of the angle of the antiphase boundaries (APBs) with Sb amount. The microstructure is assessed through high angle annular dark field (HAADF) experiments and image simulation revealing Z-contrast loss in APBs due to the superposition of ordered domains.
Direct nucleation, morphology and compositional tuning of InAs1-x Sb x nanowires on InAs (111) B substrates.[Pubmed:28346221]
Nanotechnology. 2017 Apr 21;28(16):165601.
III-V ternary nanowires are interesting due to the possibility of modulating their physical and material properties by tuning their material composition. Amongst them InAs1-x Sb x nanowires are good candidates for applications such as Infrared detectors. However, this material has not been grown directly from substrates, in a large range of material compositions. Since the properties of ternaries are alterable by tuning their composition, it is beneficial to gain access to a wide range of composition tunability. Here we demonstrate direct nucleation and growth of InAs1-x Sb x nanowires from Au seed particles over a broad range of compositions (x = 0.08-0.75) for different diameters and surface densities by means of metalorganic vapor phase epitaxy. We investigate how the nucleation, morphology, solid phase Sb content, and growth rate of these nanowires depend on the particle dimensions, and on growth conditions such as the vapor phase composition, V/III ratio, and temperature. We show that the solid phase Sb content of the nanowires remains invariant towards changes of the In precursor flow. We also discuss that at relatively high In flows the growth mechanism alters from Au-seeded to what is referred to as semi In-seeded growth. This change enables growth of nanowires with a high solid phase Sb content of 0.75 that are not feasible via Au-seeded growth. Independent of the growth conditions and morphology, we report that the nanowire Sb content changes over their length, from lower Sb contents at the base, increasing to higher amounts towards the tip. We correlate the axial Sb content variations to the axial growth rate measured in situ. We also report spontaneous core-shell formation for Au-seeded nanowires, where the core is Sb-rich in comparison to the Sb-poor shell.
Differing Mechanisms of Death Induction by Fluorinated Taxane SB-T-12854 in Breast Cancer Cells.[Pubmed:28373418]
Anticancer Res. 2017 Apr;37(4):1581-1590.
BACKGROUND/AIM: Classical taxanes are routinely used in cancer therapy. In this study, mechanisms involved in death induction by the novel fluorine-containing taxane SB-T-12854 were investigated. MATERIALS AND METHODS: We employed breast cancer SK-BR-3, MCF-7 and T47D cell lines to assess activation of individual caspases, changes in the expression of proteins of the Bcl-2 family, and the release of pro-apoptotic factors from mitochondria into the cytosol after SB-T-12854 treatment. RESULTS: Caspase-2, -8, and -9 were activated in SK-BR-3 and MCF-7 cells. Only caspase-8 was activated in T47D cells. Caspase-7 and -6 were activated in all tested cells while caspase-3 was activated only in SK-BR-3 cells. Pro-apoptotic Bad protein seems to be important for cell death induction in all tested cells. Anti-apoptotic Bcl-2 and pro-apoptotic Bim, Bok, Bid and Bik seem to be also associated with cell death induction in some of the tested cells. The mitochondrial apoptotic pathway was significantly activated in association with the release of cytochrome c and Smac from mitochondria, but only in SK-BR-3 cells, not in MCF-7 and T47D cells. CONCLUSION: Cell death induced by SB-T-12854, in the tested breast cancer cells, differs regarding activation of caspases, changes in levels of pro-apoptotic and anti-apoptotic proteins of the Bcl-2 family and activation of the mitochondrial apoptotic pathway.
Critical evaluation of strategies for single and simultaneous determinations of As, Bi, Sb and Se by hydride generation inductively coupled plasma optical emission spectrometry.[Pubmed:28340714]
Talanta. 2017 May 15;167:217-226.
A systematic study of hydride generation (HG) of As, Bi, Sb and Se from solutions containing As(III), As(V), Bi(III), Sb(III), Sb(V), Se(IV) and Se(VI) was presented. Hydrides were generated in a gas-liquid phase separation system using a continuous flow vapor generation accessory (VGA) by mixing acidified aqueous sample, HCl and sodium borohydride reductant (NaBH4) solutions on-line. For detection, a simultaneous axially viewed inductively coupled plasma optical emission spectrometer (ICP-OES) was applied. Effects of the HCl concentration (related to sample and additional acid solutions) and type of the pre-reducing agents used for reduction of As(V), Sb(V) and Se(VI) into As(III), Sb(III) and Se(IV) on the analytical responses of As, Bi, Sb and Se were studied and discussed. Two compromised HG reaction conditions for simultaneous measurements of As+Bi+Sb (CC1) or As+Sb+Se (CC2) were established. It was found that choice of the pre-reductant prior to formation of the hydrides is critical in obtaining the dependable results of the analysis. Accordingly, for a As(III)+As(V)+Bi(III)+Sb(III)+Sb(V) mixture and using CC1, thiourea/thiourea-ascorbic acid interfered in Bi determination and hence, total As+Sb could be measured. If L-cysteine/L-cysteine-ascorbic acid were used, measurements of total Bi+Sb was possible in these HG reaction conditions. For a As(III)+As(V)+Sb(III)+Sb(V)+Se(IV)+Se(VI) mixture and using CC2, thiourea/thiourea-ascorbic acid and L-cysteine/L-cysteine-ascorbic acid influenced HG of Se but ensured total As+Sb determination. In contrast, heating a sample solution with HCl, although did not pre-reduce As(V) and Sb(V), assured quantitative reduction of Se(VI) to Se(IV). Finally, considering all favorable pre-reducing and HG conditions, methodologies for reliable determination of total As, Bi, Sb and Se by HG-ICP-OES were proposed. Strategies for single-, two- and three-element measurements were evaluated and validated, obtaining the detection limits (DLs) below 0.1ngg(-1) and precision typically in the range of 1.4-3.9% RSD.
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.[Pubmed:10737744]
J Med Chem. 2000 Mar 23;43(6):1123-34.
The evolution, synthesis, and biological activity of a novel series of 5-HT(2C) receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT(2C) affinity and selectivity over 5-HT(2A) receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with additional selectivity over the closely related 5-HT(2B) receptor. Compounds from this series are inverse agonists at the human cloned 5-HT(2C) receptor, completely abolishing basal activity in a functional assay. The new series have reduced P450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biological profile, 32 (SB-228357) and 40 (SB-243213) have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.[Pubmed:10188965]
Br J Pharmacol. 1999 Feb;126(3):572-4.
Atypical neuroleptics produce fewer extrapyramidal side-effects (EPS) than typical neuroleptics. The pharmacological profile of atypical neuroleptics is that they have equivalent or higher antagonist affinity for 5-HT2 than for dopamine D2 receptors. Our aim was to identify which 5-HT2 receptor contributed to the atypical profile. Catalepsy was defined as rats remaining immobile over a horizontal metal bar for at least 30 s, 90 min after dosing. Radioligand binding assays were carried out with homogenates of human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors expressed in Human Embryo Kidney (HEK293) cells. Haloperidol (1.13 mg kg(-1) i.p.) induced catalepsy in all experiments. The selective 5-HT2C/2B receptor antagonist, SB-228357 (0.32-10 mg kg(-1) p.o.) significantly reversed haloperidol-induced catalepsy whereas the 5-HT2A and 5-HT2B receptor antagonists, MDL-100907 (0.003-0.1 mg kg(-1) p.o.) and SB-215505 (0.1-3.2 mg kg(-1) p.o.) respectively did not reverse haloperidol-induced catalepsy. The data suggest a role for 5-HT2C receptors in the anticataleptic action of SB-228357.