HG-10-102-01

Name: HG-10-102-01
Brand: MedChemExpress
SKU: HY-13488
Rating: 4.5 (1 reviews)

Cat. No.: HY-13488 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC₅₀ values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC₅₀ values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.

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

HG-10-102-01 Chemical Structure

CAS No. : 1351758-81-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE HG-10-102-01

•Harvard Medical School LINCS LIBRARY

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

View All Isoforms

MNK1 MNK2 MNK

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 3.2 nM (LRRK2[G2019S]), 20.3 nM (wild-type LRRK2), 95.9 nM (LRRK2[G2019S+A2016T], 153.7 nM (LRRK2[A2016T]), 0.6 μM (MNK2), 2.1 μM (MLK1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	153.7 nM Compound: 4, HG-10-102-01	Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method	[PMID: 23066449]
HEK293	IC₅₀	20.3 nM Compound: 4, HG-10-102-01	Inhibition of LRRK2 expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method Inhibition of LRRK2 expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method	[PMID: 23066449]
HEK293	IC₅₀	3.2 nM Compound: 4, HG-10-102-01	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method	[PMID: 23066449]
HEK293	IC₅₀	95.9 nM Compound: 4, HG-10-102-01	Inhibition of LRRK2 G2019S/A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method Inhibition of LRRK2 G2019S/A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method	[PMID: 23066449]

In Vitro

HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant^[1].

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

Western Blot Analysis^[1]

Cell Line:	HEK293 cells, Mouse Swiss 3T3 cells and Mouse embryonic fibroblast cells
Concentration:	0, 0.01, 0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time:	90 min
Result:	Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. Induced similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells and mouse embryonic fibroblast cells.

In Vivo

HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice^[1].
HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure^[1].

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

Animal Model:	Wild type male C57BL/6 mice^[1]
Dosage:	0, 3, 10, 30, 50, and 100 mg/kg
Administration:	IP, once
Result:	Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.

Animal Model:

Wild type male C57BL/6 mice^[1]

Dosage:

1 mg/kg (IV); 10 mg/kg (PO)

Administration:

IV, PO; once (Pharmacokinetic Analysis)

Result:

Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice^[1].

	IV (1 mg/kg)	PO (10 mg/kg)
T_max (h)		0.25
C_max (ng/mL)	1330	1241
AUC_last (ng/mL∗h)	74.85	502.34
AUC_INF (ng/mL∗h)	75.06	503.41
T_1/2 (h)	0.13
CL (mL/min/kg)	222.04
Vss (L/kg)	1.68
F (%)		67

Molecular Weight

377.83

Formula

C₁₇H₂₀ClN₅O₃

CAS No.

1351758-81-0

Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C(N2CCOCC2)=O)=CC=C1NC3=NC(NC)=C(Cl)C=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (132.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6467 mL	13.2335 mL	26.4669 mL
5 mM	0.5293 mL	2.6467 mL	5.2934 mL
10 mM	0.2647 mL	1.3233 mL	2.6467 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.55%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (253 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Choi HG, et al. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. [Content Brief]

[2]. Wang M, et al. Synthesis of [11C]HG-10-102-01 as a new potential PET agent for imaging of LRRK2 enzyme in Parkinson's disease. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1351-1355. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6467 mL	13.2335 mL	26.4669 mL	66.1673 mL
	5 mM	0.5293 mL	2.6467 mL	5.2934 mL	13.2335 mL
	10 mM	0.2647 mL	1.3233 mL	2.6467 mL	6.6167 mL
	15 mM	0.1764 mL	0.8822 mL	1.7645 mL	4.4112 mL
	20 mM	0.1323 mL	0.6617 mL	1.3233 mL	3.3084 mL
	25 mM	0.1059 mL	0.5293 mL	1.0587 mL	2.6467 mL
	30 mM	0.0882 mL	0.4411 mL	0.8822 mL	2.2056 mL
	40 mM	0.0662 mL	0.3308 mL	0.6617 mL	1.6542 mL
	50 mM	0.0529 mL	0.2647 mL	0.5293 mL	1.3233 mL
	60 mM	0.0441 mL	0.2206 mL	0.4411 mL	1.1028 mL
	80 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8271 mL
	100 mM	0.0265 mL	0.1323 mL	0.2647 mL	0.6617 mL

HG-10-102-01 Related Classifications

Neurological Disease

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.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

HG-10-102-01

Customer Review

HG-10-102-01 Related Antibodies

1 Publications Citing Use of MCE HG-10-102-01

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

HG-10-102-01 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

HG-10-102-01 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report