RO-275

Cat. No.: HY-160505 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

RO-275 (compound 29) is a potent, selective and orally active HCN1 inhibitor with IC₅₀ values of 0.046, 14.3, 4.6, 13.9 µM for HCN1, HCN2, HCN3, HCN4, respectively. RO-275 rescues decremented working memory. RO-275 has the potential for the research of cognitive dysfunction in brain disorder.

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

RO-275 Chemical Structure

CAS No. : 2648837-04-9

Size	Price	Stock	Quantity
5 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC₅₀: 0.046 µM (HCN1); 14.3 µM (HCN2); 4.6 µM (HCN3); 13.9 µM (HCN4)^[1]

In Vivo

RO-275 (3, 10, 30 mg/kg; i.p.) rescues decremented working memory in rats^[2].

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

Animal Model:	Male Sprague Dawley rats^[2]
Dosage:	3, 10, 30 mg/kg
Administration:	I.p.
Result:	Improved performance in a translationally relevant touchscreen task of working memory (WM), tended to improve performance, but only at the longest delay of 6 s at the 10 mg/kg dose level, and led to a significant reduction in incorrect trials at 30 mg/kg in trial-unique, delayed non-matching-to-location (TUNL).

Molecular Weight

351.79

Formula

C₁₈H₁₄ClN₅O

CAS No.

2648837-04-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC(C#CC2=C(C)C(Cl)=NC=C2)=C(C)N1C3=CC=CN=C3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (14.21 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	2.8426 mL	14.2130 mL	28.4260 mL
5 mM	0.5685 mL	2.8426 mL	5.6852 mL
10 mM	0.2843 mL	1.4213 mL	2.8426 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)

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: ≥ 0.5 mg/mL (1.42 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.42 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.42 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 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 (5.0 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).

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: ≥99.0%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) HNMR (688 KB) RP-HPLC (769 KB)

Handling Instructions (2659 KB)

References

[1]. Bjoern Bartels, et al. Alkynyl-(heteroaryl)-carboxamide hcn1 inhibitors. WO2021110574A1.

[2]. Harde E, et al. Selective and brain-penetrant HCN1 inhibitors reveal links between synaptic integration, cortical function, and working memory. Cell Chem Biol. 2024 Mar 21;31(3):577-592.e23. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8426 mL	14.2130 mL	28.4260 mL	71.0651 mL
	5 mM	0.5685 mL	2.8426 mL	5.6852 mL	14.2130 mL
	10 mM	0.2843 mL	1.4213 mL	2.8426 mL	7.1065 mL

RO-275 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.

Keywords:

RO-2752648837-04-9RO275RO 275HCN ChannelHyperpolarization activated cyclic nucleotide gated channelssynapticworking memorybrain disorderInhibitorinhibitorinhibit

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