HG-10-102-01 |
| Catalog No.GC13098 |
HG-10-102-01 est un inhibiteur LRRK2 très puissant, sélectif et pénétrable dans le cerveau, avec des valeurs IC50 de 20,3 et 3,2 nM contre LRRK2 de type sauvage et LRRK2 [G2019S], respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1351758-81-0
Sample solution is provided at 25 µL, 10mM.
HG-10-102-01 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with the IC50 values of 20.3nM and 3.2nM for wild type LRRK2 and LRRK2 [G1019S], respectively [1].
HG-10-102-01 has shown the potent and selective inhibitor of LRRK2 with the IC50 values of 20.3nM, 153.7nM, 95.9nM and 3.2nM for wild type LRRK2, LRRK2 [A2016T], LRRK2 [G2019S+A1016T] and LRRK2 [G1019S], respectively. In addition, HG-10-102-01 has been reported to induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 [G2019S] stably transfected into HEK 293 cells. Moreover, it has been demonstrated that increasing doses of HG-10-102-01 led to similar dephosphorylation of endogenous LRRK2 at Ser910 and Ser935 in HEK293 cells, mouse Swiss 3T3 cells and mouse embryonic fibroblast cells [1].
References:
[1] Choi HG1, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. Epub 2012 Jun 18.
| Cas No. | 1351758-81-0 | SDF | |
| Chemical Name | (E)-(4-((5-chloro-6-(methylimino)-1,6-dihydropyrimidin-2-yl)amino)-2-methoxyphenyl)(morpholino)methanone | ||
| Canonical SMILES | C/N=C(N1)\C(Cl)=CN=C1NC2=CC(OC)=C(C(N3CCOCC3)=O)C=C2 | ||
| Formula | C17H20ClN5O3 | M.Wt | 377.83 |
| Solubility | ≥ 18.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6467 mL | 13.2335 mL | 26.4669 mL |
| 5 mM | 529.3 μL | 2.6467 mL | 5.2934 mL |
| 10 mM | 264.7 μL | 1.3233 mL | 2.6467 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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