(S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate
- CAS No.
- 1788063-52-4
- Chemical Name:
- (S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate
- Synonyms
- (S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate;(S)-5-cyclopropyl-4-((1-(1-(3,5-dichlorophenyl)ethyl)piperidin-4-yl)methoxy)-2-fluoro-N-(methylsulfonyl)benzamide;Benzamide, 5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]-4-piperidinyl]methoxy]-2-fluoro-N-(methylsulfonyl)-
- CBNumber:
- CB93048677
- Molecular Formula:
- C25H29Cl2FN2O4S
- Molecular Weight:
- 543.48
- MDL Number:
- MOL File:
- 1788063-52-4.mol
(S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate Properties
Density | 1.358±0.06 g/cm3(Predicted) |
---|---|
storage temp. | Store at -20°C |
pka | 3.41±0.40(Predicted) |
form | Solid |
color | White to off-white |
FDA UNII | 72GO7NL642 |
(S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate Chemical Properties,Uses,Production
Uses
GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7[1].
in vivo
GDC-0310 shows substantially improved Nav selectivity and ADME properties[1].
GDC-0310 exhibits t1/2 values of 5 h, 46 h and 4.4 h in rat (5 mg/kg, iv), dog (1 mg/kg, iv) and cynomolgus monkeys (2 mg/kg, iv), respectively[1].
IC 50
hNav1.4: 3.4 nM (IC50); hNav1.2: 38 nM (IC50); hNav1.6: 198 nM (IC50); hNav1.1: 202 nM (IC50); hNav1.5: 551 nM (IC50); Nav1.7: 0.6 nM (IC50)
References
[1] Brian S Safina, et al. Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310. J Med Chem. 2021 Mar 25;64(6):2953-2966. DOI:10.1021/acs.jmedchem.1c00049
[2] Lei Xu, et al. Voltage-gated sodium channels: structures, functions, and molecular modeling. Drug Discov Today. 2019 Jul;24(7):1389-1397. DOI:10.1016/j.drudis.2019.05.014
(S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate Preparation Products And Raw materials
Raw materials
Preparation Products
(S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19961 | 58 |
Shanghai Chaolan Chemical Technology Center | 021-QQ:65489617 15618227136 | Sales@ATKchemical.com | China | 9848 | 58 |
Shanghai Star Pharmaceutical Chemical Technology Co., Ltd. | 021-58521787 17701827760 | starpharmsh@gmail.com | China | 292 | 58 |
Birdo (Shanghai) Medical Technology Co., Ltd. | 021-58099077-8041 18601625411 | sales@birdotech.com | China | 10000 | 58 |
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 997 | 58 |
Shanghai Merlot Chemical Co., LTD | 15821661757 | 226174156@qq.com | China | 476 | 58 |
Shanghai Tachizaki Biomedical Research Center | 18014399201 | sales@chemlab-tachizaki.com | China | 2680 | 58 |
Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5840 | 58 |