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  3. LRRK2-IN-7

LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.

For research use only. We do not sell to patients.

LRRK2-IN-7 Chemical Structure

LRRK2-IN-7 Chemical Structure

CAS No. : 2307277-93-4

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5 mg USD 720 In-stock
10 mg USD 1150 In-stock
25 mg USD 2450 In-stock
50 mg USD 3880 In-stock
100 mg USD 6200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of LRRK2-IN-7:

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  • Purity & Documentation

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Description

LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1].

IC50 & Target

IC50: 0.9 nM (LRRK2 Kinase)[1]

In Vitro

LRRK2-IN-7 (compound 25) is both a mouse breast cancer resistance protein (BCRP) substrate (mouse/human BCRP) and a potent human BCRP inhibitor (BCRP IC50 = 0.12 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In a 7 day rat dose limiting toxicity study, LRRK2-IN-7 (compound 25) is tolerated with no significant histopathology findings up to 100 mg/kg once a day (AUCtot = 330 μM·h)[1].
In an acute (2 h) rat PK/PD study, LRRK2-IN-7 (compound 25) demonstrates a dose-dependent decrease in LRRK2 pS935 in rat brain striatum with an EC50 = 0.18 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

414.50

Formula

C24H26N6O

CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

CC(C)(O)[C@@H]1CCN(C1)C2=NC=NC(N3C4=CC([C@@]5(CC56CC6)C#N)=CC=C4C=N3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (241.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4125 mL 12.0627 mL 24.1255 mL
5 mM 0.4825 mL 2.4125 mL 4.8251 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4125 mL 12.0627 mL 24.1255 mL 60.3136 mL
5 mM 0.4825 mL 2.4125 mL 4.8251 mL 12.0627 mL
10 mM 0.2413 mL 1.2063 mL 2.4125 mL 6.0314 mL
15 mM 0.1608 mL 0.8042 mL 1.6084 mL 4.0209 mL
20 mM 0.1206 mL 0.6031 mL 1.2063 mL 3.0157 mL
25 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4125 mL
30 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0105 mL
40 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5078 mL
50 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
60 mM 0.0402 mL 0.2010 mL 0.4021 mL 1.0052 mL
80 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7539 mL
100 mM 0.0241 mL 0.1206 mL 0.2413 mL 0.6031 mL
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LRRK2-IN-7 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LRRK2-IN-7
Cat. No.:
HY-152107
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