[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0]

Request For Quotation
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Suppliers list
Company Name: Nantong QuanYi Biotechnology Co., Ltd  Gold
Tel: 0513-66337626 18051384581
Email: sales@chemhifuture.com
Company Name: Soochow Chirally Material Science and Technology Co.,Ltd  Gold
Tel: 0512-66834346 17751187418
Email: sales@krl-tech.com
Company Name: Nantong Hanfang Biotechnology Co. , Ltd.  Gold
Tel: hanfangpharma@126.com 18017580634
Email: hanfangpharma@126.com
Company Name: WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.  
Tel: 17702719238
Email: sales@sun-shinechem.com
Company Name: Nanjing Chemlin Chemical Co., Ltd  
Tel: 025-83697070 13770331960
Email: info@chemlin.com.cn
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Basic information
Product Name:[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0]
Synonyms:[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0];Methanone, [5-(methylsulfonyl)-2-[(1R)-2,2,2-trifluoro-1-methylethoxy]phenyl][(1R,5R)-1-[5-(trifluoromethyl)-3-isoxazolyl]-3-azabicyclo[3.1.0]hex-3-yl]-;Iclepertin (BI-425809);[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo;(5-(Methylsulfonyl)-2-(((R)-1,1,1-trifluoropropan-2-yl)oxy)phenyl)((1R,5R)-1-(5-(trifluoromethyl)isoxazol-3-yl)-3-azabicyclo[3.1.0]hexan-3-yl)methanone;(1R,5R)-3-(5-methanesulfonyl-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}benzoyl)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hexane;Iclepertin
CAS:1421936-85-7
MF:C20H18F6N2O5S
MW:512.42
EINECS:812-974-1
Product Categories:
Mol File:1421936-85-7.mol
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Structure
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Chemical Properties
Boiling point 605.2±55.0 °C(Predicted)
density 1.508±0.06 g/cm3(Predicted)
solubility Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml
form Solid
pka-2.86±0.40(Predicted)
color White to off-white
InChIKeyMYHDQTVHHMSLEF-DDBGAENHSA-N
SMILESC(C1=CC(S(C)(=O)=O)=CC=C1O[C@H](C)C(F)(F)F)(N1C[C@@]2([H])[C@](C3C=C(C(F)(F)F)ON=3)(C2)C1)=O
Safety Information
MSDS Information
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Usage And Synthesis
Uses[5-(Methylsulfonyl)-2-[(1R)-2,2,2-trifluoro-1-methylethoxy]phenyl][(1R,5R)-1-[5-(trifluoromethyl)-3-isoxazolyl]-3-azabicyclo[3.1.0]hex-3-yl]-methanone is a solid form of GlyT1 inhibitor.
in vivo

Single oral administration of Iclepertin induced a dose-dependent increase of glycine cerebrospinal fluid (CSF) levels. Oral administration of Iclepertin in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg), relative to vehicle[1].

IC 50GLT1: 5.2 mM (IC50, In rat primary neurons ); GLT1: 5 nM (IC50, In human SK-N-MC cells)
References[1] HOLGER ROSENBROCK. Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies[J]. Cts-Clinical and Translational Science, 2018, 11 6: 616-623. DOI: 10.1111/cts.12578
[2] ROSENBROCK H, DORNER‐CIOSSEK C, GIOVANNINI R, et al. Effects of the Glycine Transporter-1 Inhibitor Iclepertin (BI 425809) on Sensory Processing, Neural Network Function, and Cognition in Animal Models Related to Schizophrenia[J]. The Journal of Pharmacology and Experimental Therapeutics, 2022, 24 1: 0. DOI: 10.1124/jpet.121.001071
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] Preparation Products And Raw materials
Tag:[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0](1421936-85-7) Related Product Information
[5-Methanesulfonyl-2-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[(1R,5R)-1-(5-trifluoromethyl-isoxazol-3-yl)-3-aza-bicyclo[3.1.0] (S)-methyl 3-(1-benzyl-1H-imidazol-4-yl)-2-(6-(benzyloxy)-5-methoxy-1H-indole-2-carboxamido)propanoate SB-699551 (hydrochloride) GBR 12783 dihydrochloride Swertisin Glutaurine