RO2959 monohydrochloride

Name: RO2959 monohydrochloride
Brand: MedChemExpress
SKU: HY-113618B
Rating: 4.5 (1 reviews)

Cat. No.: HY-113618B Purity: 98.21%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.

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

RO2959 monohydrochloride Chemical Structure

CAS No. : 2309172-44-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1750	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of RO2959 monohydrochloride:

RO2959 hydrochloride Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CRAC channel

402 nM (IC₅₀)

Orai1/Stim1 channels

25 nM (IC₅₀)

IL-2

In Vitro

RO2959 inhibits Orai1 and Orai3 with IC₅₀ values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC₅₀ value of 265 nM^[1].
RO2959 is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4⁺ T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction)^[1].

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

Molecular Weight

463.93

Formula

C₂₁H₂₀ClF₂N₅OS

CAS No.

2309172-44-7

Appearance

Solid

Color

Light brown to brown

SMILES

O=C(NC1=NC=C(C2=C(C)CCN(C3=NC=C(C)S3)C2)N=C1)C4=C(F)C=CC=C4F.[H]Cl

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 : 25 mg/mL (53.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1555 mL	10.7775 mL	21.5550 mL
5 mM	0.4311 mL	2.1555 mL	4.3110 mL
10 mM	0.2155 mL	1.0777 mL	2.1555 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

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: 2.08 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 98.21%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (248 KB) RP-HPLC (250 KB) MS (71 KB)

Handling Instructions (2659 KB)

References

[1]. Gang Chen, et al. Characterization of a Novel CRAC Inhibitor That Potently Blocks Human T Cell Activation and Effector Functions. Mol Immunol. 2013 Jul;54(3-4):355-67. [Content Brief]

[2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1555 mL	10.7775 mL	21.5550 mL	53.8874 mL
	5 mM	0.4311 mL	2.1555 mL	4.3110 mL	10.7775 mL
	10 mM	0.2155 mL	1.0777 mL	2.1555 mL	5.3887 mL
	15 mM	0.1437 mL	0.7185 mL	1.4370 mL	3.5925 mL
	20 mM	0.1078 mL	0.5389 mL	1.0777 mL	2.6944 mL
	25 mM	0.0862 mL	0.4311 mL	0.8622 mL	2.1555 mL
	30 mM	0.0718 mL	0.3592 mL	0.7185 mL	1.7962 mL
	40 mM	0.0539 mL	0.2694 mL	0.5389 mL	1.3472 mL
	50 mM	0.0431 mL	0.2155 mL	0.4311 mL	1.0777 mL