3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate
- CAS No.
- 1192189-69-7
- Chemical Name:
- 3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate
- Synonyms
- LX7101;CS-2042;LX7101 HCL;LX7101 (LX-7101);LX7101 (3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo;inhibit,Inhibitor,LX 7101,LX7101,Rho-associated protein kinase,Rho-associated kinase,ROCK,LX-7101,Rho-kinase,ROK;3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate;3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl N.N-dimethylcarbamate;LX7101 (3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate;N,N-Dimethylcarbamic acid 3-[[[4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]carbonyl]amino]phenyl ester
- CBNumber:
- CB42638542
- Molecular Formula:
- C23H29N7O3
- Molecular Weight:
- 451.52
- MDL Number:
- MOL File:
- 1192189-69-7.mol
3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate Properties
Density | 1.327±0.06 g/cm3(Predicted) |
---|---|
storage temp. | Store at -20°C |
solubility | insoluble in H2O; insoluble in EtOH; insoluble in DMSO |
form | solid |
pka | 13.96±0.70(Predicted) |
color | White to off-white |
FDA UNII | 74B3C4ZT96 |
3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-5103 | LX7101 99.57% | 1192189-69-7 | 2mg | $100 | 2021-12-16 | Buy |
ChemScene | CS-5103 | LX7101 99.57% | 1192189-69-7 | 5mg | $200 | 2021-12-16 | Buy |
ApexBio Technology | B5863 | LX7101HCL | 1192189-69-7 | 2mg | $205 | 2021-12-16 | Buy |
ChemScene | CS-5103 | LX7101 99.57% | 1192189-69-7 | 10mg | $350 | 2021-12-16 | Buy |
ApexBio Technology | B5863 | LX7101HCL | 1192189-69-7 | 5mg | $378 | 2021-12-16 | Buy |
3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate Chemical Properties,Uses,Production
Biological Activity
lim-kinases 1 and 2 (limk1 and limk2) regulate cytoskeletal dynamics by phosphorylating and deactivating cofilin, a protein that depolymerizes actin filaments. rock, a kinase upstream of limk in the signaling cascade that regulates actin filament dynamics, are being investigated in the clinic for reduction of iop through relaxation of the trabecular meshwork. lx7101 is a dual lim-kinase and rock inhibitor for the treatment of glaucoma.
in vitro
lx7101 proved significantly more selective for limk2. in addition, lx7101 was screened against a panel of 403 kinases. moderate selectivity was observed in this screen (34 assays including limk2 and rock2 indicated that the kd is most likely <1 μm) [1].
in vivo
at a well-tolerated dose, lx7101 achieved additional reduction of iop compared to the 0.1% formulation and demonstrated a long duration of action, with iop not returning to baseline until more than 8 h postdose. more critically, lx7101 produced a significantly greater reduction of iop than either timolol or latanoprost [1].
IC 50
4.3, 32, 69 and 32 nm for limk2, kimk1, rock1 and rock2, respectivley
References
[1] harrison ba, almstead zy, burgoon h, gardyan m, goodwin nc, healy j, liu y, mabon r, marinelli b, samala l, zhang y, stouch tr, whitlock na, gopinathan s, mcknight b, wang s, patel n, wilson ag, hamman bd, rice ds, rawlins db. discovery and development of lx7101, a dual lim-kinase and rock inhibitor for the treatment of glaucoma. acs med chem lett. 2014 nov 24;6(1):84-8.
3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28172 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52924 | 58 |
Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39004 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2922 | 55 | |
BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 14055 | 65 |
Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7552 | 61 |
1192189-69-7(3-(4-(aMinoMethyl)-1-(5-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidine-4-carboxaMido)phenyl diMethylcarbaMate)Related Search:
1of4