ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
- Product Name
- ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
- CAS No.
- 1215849-96-9
- Chemical Name
- ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
- Synonyms
- FSC 231 (FSC231);ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate;(E)-ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate;Ethyl (E)-(2-cyano-3-(3,4-dichlorophenyl)acryloyl)carbamate;Ethyl?N-[(2E)-2-cyano-3-(3,4-dichlorophenyl)-1-oxo-2-propen-1-yl]carbamate;Carbamic acid, N-[(2E)-2-cyano-3-(3,4-dichlorophenyl)-1-oxo-2-propen-1-yl]-, ethyl ester
- CBNumber
- CB13525417
- Molecular Formula
- C13H10Cl2N2O3
- Formula Weight
- 313.14
- MOL File
- 1215849-96-9.mol
ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate Property
- Melting point:
- 175-178 °C(Solv: toluene (108-88-3))
- Density
- 1.404±0.06 g/cm3(Predicted)
- storage temp.
- RT
- solubility
- Soluble in DMSO (up to 35 mg/ml with warming) or in Ethanol (up to 18 mg/ml with warming)
- pka
- 7.83±0.46(Predicted)
- form
- solid
- color
- Yellow
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate Chemical Properties,Usage,Production
Description
FSC-231 (1215849-96-9) is the first small-molecule inhibitor of the PDZ domain in protein interacting with C kinase 1 (PICK1). Binds to PICK1 PDZ domain with affinity similar to that of the endogenous peptide ligands (Ki~10.1 μM). Does not bind to PDZ domains of postsynaptic density protein 95 (PSD-95) nor glutamate receptor interacting protein 1 (GRIP1). Pretreatment of cultured hippocampal neurons inhibits coimmunoprecipitation of the AMPA receptor GluR2 subunit with PICK1. FSC231 accelerated recycling of fluorophore-tagged GluR2 in hippocampal neurons after internalization in response to NMDA receptor activation. Blocks the expression of both long-term depression and long-term potentiation.1,2 Attenuates cocaine seeking in a rodent model.3 Blocks PICK1-induced anti-inflammatory effect in acute liver injury.4
Uses
FSC231 is a PSD‐95/DLG/ZO‐1 (PDZ) domain inhibitor of PICK1. FSC231 has analgesic effects[1].
in vivo
FSC231 (78.40 μg/kg in total, daily, seven times, i.p., 3 h before Paclitaxel) alleviates the Paclitaxel (HY-B0015)‐induced neuralgia of rats[1].
FSC231 (39.2μg/kg/day, i.p., for 4 weeks) inhibits the development of diabetic cardiomyopathy in rats by inhibiting ROS generation and apoptosis partly via PICK1/eNOS/cGMP pathway[3].
| Animal Model: | Paclitaxel (HY-B0015)‐induced neuralgia of rats[1] |
| Dosage: | 78.40 μg/kg in total |
| Administration: | i.p., daily, seven times, completed at 3 h before Paclitaxel |
| Result: | Reversed the changes of inflammatory cytokines (IL‐6, TNF‐α and IL‐10). Inhibited the phosphorylation levels of GSK‐3β and ERK1/2. |
References
[1] THOR S THORSEN. Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2010: 413-418. DOI:10.1073/pnas.0902225107
[2] QINGPING TANG . Willed-movement training reduces motor deficits and induces a PICK1-dependent LTD in rats subjected to focal cerebral ischemia[J]. Behavioural Brain Research, 2013, 256: Pages 481-487. DOI:10.1016/j.bbr.2013.08.039
[3] HEATH D SCHMIDT. Stimulation of mGluR5 in the accumbens shell promotes cocaine seeking by activating PKC gamma.[J]. Journal of Neuroscience, 2013, 33 35: 14160-14169. DOI:10.1523/jneurosci.2284-13.2013
[4] JUAN XIE . PICK1 confers anti-inflammatory effects in acute liver injury via suppressing M1 macrophage polarization[J]. Biochimie, 2016, 127: Pages 121-132. DOI:10.1016/j.biochi.2016.05.002
ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate Preparation Products And Raw materials
Raw materials
Preparation Products
ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate Suppliers
- Tel
- 0512-87182056 18013166090
- Fax
- 0512-87182056
- lingling.qi@yacoo.com.cn
- Country
- China
- ProdList
- 6295
- Advantage
- 60
- Tel
- 13816613772
- Fax
- QQ: 12922499
- huahero21@sina.com
- Country
- China
- ProdList
- 2519
- Advantage
- 55
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9505
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 4887
- Advantage
- 58
- Tel
- 0371-86658258；
- Fax
- QQ：3311217266
- info@kehobio.com
- Country
- China
- ProdList
- 2747
- Advantage
- 58
- Tel
- 400-1647117 13681763483
- product02@bidepharm.com
- Country
- China
- ProdList
- 59936
- Advantage
- 58
- Tel
- 13720134139 086-15871494362 13720134139
- orders@jknbiochem.com
- Country
- China
- ProdList
- 7047
- Advantage
- 58
- Tel
- 17721492509 17721492509
- 460170712@qq.com
- Country
- China
- ProdList
- 4840
- Advantage
- 58
- Tel
- 15002134094
- marketing@targetmol.cn
- Country
- China
- ProdList
- 29431
- Advantage
- 58
- Tel
- 18122215013
- 780229652@qq.com
- Country
- China
- ProdList
- 1359
- Advantage
- 58