JH-II-127 |
Catalog No.GC19205
One-Click Copy Product Info
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JH-II-127 es un inhibidor de LRRK2 permeable al cerebro, selectivo, altamente potente y activo por vÍa oral, con IC50 de 6, 2 y 48 nM para LRRK2 y LRRK2-G2019S de tipo salvaje y LRRK2-A2016T mutante.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1700693-08-8
Sample solution is provided at 25 µL, 10mM.
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JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 uM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.
References:
[1]. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-589.
| Cas No. | 1700693-08-8 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(NC2=NC3=NC=C(Cl)C3=C(NC)N2)C(OC)=C1)N4CCOCC4 | ||
| Formula | C19H21ClN6O3 | M.Wt | 416.86 |
| Solubility | DMSO : ≥ 30 mg/mL (71.97 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3989 mL | 11.9944 mL | 23.9889 mL |
| 5 mM | 479.8 μL | 2.3989 mL | 4.7978 mL |
| 10 mM | 239.9 μL | 1.1994 mL | 2.3989 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)