Belumosudil mesylate (Synonyms: KD025 mesylate; SLx-2119 mesylate)

Name: Belumosudil mesylate
Brand: MedChemExpress
SKU: HY-15307A
Rating: 5.0 (26 reviews)

Cat. No.: HY-15307A Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

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Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

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

Belumosudil mesylate Chemical Structure

CAS No. : 2109704-99-4

Size	Price	Stock	Quantity
1 mg	USD 36	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 114	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 225	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 348	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 588	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of Belumosudil mesylate:

Belumosudil In-stock

23 Publications Citing Use of MCE Belumosudil mesylate

: Belumosudil mesylate purchased from MedChemExpress. Usage Cited in: J Autoimmun. 2018 May;89:125-138. [Abstract]; Cells are collected on day 2 for analysis of phosphorylation of Stat1, Stat3, and Stat5 using western blots.

: Belumosudil mesylate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]; Cells lysates are subjected to SDS-PAGE and immunoblotted with anti-phospho-Akt (Ser473) and total Akt antibodies. PPARγ is used as a differentiation marker, and β-tubulin and α-actin as loading controls.

: Belumosudil mesylate purchased from MedChemExpress. Usage Cited in: Medizinische Fakultät, University Goettingen. 2016 Oct.; Purified ROCK1 and ROCK2 are incubated with H1152P (3 µM) or SLx-2119 (3 µM) prior to performing the in vitro kinase assay. Shown is a representative autoradiography (n=3).

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ROCK ROCK1 ROCK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties^[1].

IC₅₀ & Target^[1]

ROCK2

105 nM (IC₅₀)

ROCK1

24 μM (IC₅₀)

In Vitro

Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays^[1].

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

In Vivo

Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males^[2].

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

Clinical Trial

Molecular Weight

548.61

Formula

C₂₇H₂₈N₆O₅S

CAS No.

2109704-99-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1.OS(=O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (18.23 mM; ultrasonic and warming and heat to 60°C; 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	1.8228 mL	9.1139 mL	18.2279 mL
5 mM	0.3646 mL	1.8228 mL	3.6456 mL
10 mM	0.1823 mL	0.9114 mL	1.8228 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 (sealed storage, away from moisture). 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)

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: ≥ 1 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.89%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (253 KB) HNMR (289 KB) LCMS (90 KB)

Handling Instructions (2659 KB)

References

[1]. Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18. [Content Brief]

[2]. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8228 mL	9.1139 mL	18.2279 mL	45.5697 mL
	5 mM	0.3646 mL	1.8228 mL	3.6456 mL	9.1139 mL
	10 mM	0.1823 mL	0.9114 mL	1.8228 mL	4.5570 mL
	15 mM	0.1215 mL	0.6076 mL	1.2152 mL	3.0380 mL

Belumosudil mesylate Related Classifications

Inflammation/Immunology

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.

Keywords:

Belumosudil2109704-99-4KD025SLx-2119KD 025KD-025SLx2119SLx 2119ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK2Anti-fibroticInhibitorinhibitorinhibit

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Belumosudil mesylate (Synonyms: KD025 mesylate; SLx-2119 mesylate)

Customer Review

Other Forms of Belumosudil mesylate:

Belumosudil mesylate Related Antibodies

23 Publications Citing Use of MCE Belumosudil mesylate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ROCK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Belumosudil mesylate Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Belumosudil mesylate Related Classifications

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