Rhosin hydrochloride

Name: Rhosin hydrochloride
Brand: MedChemExpress
SKU: HY-12646
Rating: 5.0 (40 reviews)

Cat. No.: HY-12646 Purity: 99.94%: Data Sheet
COA

SDS
Handling Instructions
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Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.

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

CAS No. : 1281870-42-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of Rhosin hydrochloride:

Rhosin In-stock

40 Publications Citing Use of MCE Rhosin hydrochloride

ELISA

RT-PCR

: Rhosin hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Sep;645(8079):244-253. [Abstract]; Rhosin hydrochloride (Rhosin) (50 μM; 5 min) inhibited RhoA activity and diminished cGMP-stimulated ROCK and MLC phosphorylation in mature BMDCs.

: Rhosin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 22;16(1):2821. [Abstract]; The RhoA inhibitor Rhosin hydrochloride (40 μM) significantly reduced the increased expression of p-MLC, α-SMA, and COL-I induced by Sema4D treatment.

: Rhosin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 14;14(1):1402. [Abstract]; Rhosin hydrochloride (Rhosin) (30 µM) blocked the increase in the activated forms of PDGF-AA in the PCK1-KO MIHA cell supernatant.

: Rhosin hydrochloride purchased from MedChemExpress. Usage Cited in: Circulation. 2021 May 4;143(18):1775-1792. [Abstract]; RhoA inhibitor Rhosin hydrochloride (Rhosin) (30 μg/100 g; respiratory tract injection; 14 d) efficiently blocked the rescue effects of GGPP after statin treatment on hypoxia-enhanced CaSR and HIMF gene expression in pulmonary arteries of rats.

: Rhosin hydrochloride purchased from MedChemExpress. Usage Cited in: Circulation. 2021 May 4;143(18):1775-1792. [Abstract]; Western blot analysis of hypoxia-altered ROCK2 phosphorylation and the effects of Rhosin hydrochloride (Rhosin) (30 μg/100 g; respiratory tract injection; 14 d) in pulmonary arteries of rats exposed to normoxia or hypoxia.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis^[1]^[2]. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability^[3].

IC₅₀ & Target

Kd: 0.4 uM (RhoA)^[1]

In Vitro

Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC₅₀ ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells^[1].

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

In Vivo

Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice^[3].
Rhosin (30 μM; bilateral, intra- Nucleus Accumbens (NAc) infusions) attenuates stress-induced social avoidance. Rhosin blocks stress-induced hyperexcitability in NAc dopamine 1 receptor medium spiny neurons (D1-MSNs). Rhosin prevents decreased excitatory transmission on NAc D1-MSNs. Rhosin enhances spine density in defeat mice^[3].

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

Animal Model:	D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background^[3]
Dosage:	40 mg/kg
Administration:	I.p.
Result:	Rhosin was systemically administered 15 min prior to defeat to block RhoA activation. While defeat significantly reduced the time that experimental mice spent interacting with a novel mouse, Rhosin administration suppressed this effect without affecting locomotor behaviors.

Molecular Weight

394.86

Formula

C₂₀H₁₉ClN₆O

CAS No.

1281870-42-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (126.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 16.67 mg/mL (42.22 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5325 mL	12.6627 mL	25.3254 mL
5 mM	0.5065 mL	2.5325 mL	5.0651 mL
10 mM	0.2533 mL	1.2663 mL	2.5325 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: ≥ 2.5 mg/mL (6.33 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.33 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 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: ≥ 2.5 mg/mL (6.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) HNMR (520 KB) RP-HPLC (242 KB)

Handling Instructions (2659 KB)

References

[1]. Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. [Content Brief]

[2]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. [Content Brief]

[3]. Francis TC, et al. The Selective RhoA Inhibitor Rhosin Promotes Stress Resiliency Through Enhancing D1-Medium Spiny Neuron Plasticity and Reducing Hyperexcitability. Biol Psychiatry. 2019;85(12):1001-1010. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.5325 mL	12.6627 mL	25.3254 mL	63.3136 mL
	5 mM	0.5065 mL	2.5325 mL	5.0651 mL	12.6627 mL
	10 mM	0.2533 mL	1.2663 mL	2.5325 mL	6.3314 mL
	15 mM	0.1688 mL	0.8442 mL	1.6884 mL	4.2209 mL
	20 mM	0.1266 mL	0.6331 mL	1.2663 mL	3.1657 mL
	25 mM	0.1013 mL	0.5065 mL	1.0130 mL	2.5325 mL
	30 mM	0.0844 mL	0.4221 mL	0.8442 mL	2.1105 mL
	40 mM	0.0633 mL	0.3166 mL	0.6331 mL	1.5828 mL
DMSO	50 mM	0.0507 mL	0.2533 mL	0.5065 mL	1.2663 mL
	60 mM	0.0422 mL	0.2110 mL	0.4221 mL	1.0552 mL
	80 mM	0.0317 mL	0.1583 mL	0.3166 mL	0.7914 mL
	100 mM	0.0253 mL	0.1266 mL	0.2533 mL	0.6331 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.