RO-275

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Description: Potent and selective HCN1 inhibitor
Chemical Name: 4-((2-Chloro-3-methylpyridin-4-yl)ethynyl)-5-methyl-1-(pyridin-3-yl)-1H-imidazole-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for RO-275

RO-275 is a potent and selective HCN1 (hyperpolarization-activated cyclic-nucleotide-gated channel 1) inhibitor (IC50 = 46 nM). It shows <100-fold selectivity over HCN2, HCN3 and HCN4. In vivo, RO-275 improves performance in a translationally relevant touchscreen task of working memory (TUNL) in rats. RO-275 is orally bioavailable and brain-penetrant.

Licensing Information

This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the RO-275 probe summary on the SGC website.

Technical Data for RO-275

M. Wt 351.79
Formula C18H14ClN5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2648837-04-9
PubChem ID 156441547
InChI Key STQKUEFQEVDNLU-UHFFFAOYSA-N
Smiles O=C(C1=NC(C#CC2=C(C)C(Cl)=NC=C2)=C(C)N1C3=CC=CN=C3)N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for RO-275

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.59 50

Preparing Stock Solutions for RO-275

The following data is based on the product molecular weight 351.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.69 mL 28.43 mL 56.85 mL
2.5 mM 1.14 mL 5.69 mL 11.37 mL
5 mM 0.57 mL 2.84 mL 5.69 mL
25 mM 0.11 mL 0.57 mL 1.14 mL

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References for RO-275

References are publications that support the biological activity of the product.

Harde et al (2024) Selective and brain-penetrant HCN1 inhibitors reveal links between synaptic integration, cortical function, and working memory. Cell.Chem.Biol. 31 577 PMID: 38042151


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Keywords: RO-275, RO-275 supplier, RO275, potent, selective, orally, bioavailable, brain-penetrant, inhibitors, inhibits, HCN1, HCN3, HCN4, working, memory, HCN, Channels, 8977, Tocris Bioscience

Citations for RO-275

Citations are publications that use Tocris products.

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