Structure
LX7101, inhibitor
LX7101
Purity
98.00%
Synonyms
LX7101; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 150mg/mL (332.21mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C23H29N7O3
SMILES
NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1
CAS Number
1192189-69-7
Target & IC50
ROCK2: ic50 10nM
LIMK2: ic50 1.6nM
LIMK1: ic50 24nM
PKA: ic50 1nM
LIMK2: ic50 1.6nM
LIMK1: ic50 24nM
PKA: ic50 1nM
In Vitro
Topical doses of LX-7101 are evaluated for tolerability in the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single-dose studies. LX-7101 is advanced to Phase-I clinical trials as intraocular pressure (IOP)-lowering agent for the treatment of glaucoma. LX-7101 shows a significant IOP reduction at time points ranging from 1 h to 6 h post-administration in rabbits[1]. LX-7101 (5%) achieved an additional reduction of IOP (5.0mMHg total reduction) compared to the 0.1% formulation. It also demonstrated a long duration of action, in the mouse IOP assay, with IOP not returning to baseline until more than 8 h postdose[2].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for LX7101, inhibitor
LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1nM).
Product Categories/Family for LX7101, inhibitor
References
Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010.
Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010.
Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the treatment,of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88.
Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the treatment,of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88.
Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010.
Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the treatment,of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88.
Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the treatment,of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88.
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Product Notes
The LX7101 (Catalog #AAA5755128) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "LX7101, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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