SAR 216471 hydrochloride

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Cat.No. 5650 - SAR 216471 hydrochloride | C28H31ClN8O3.HCl | CAS No. 1279829-64-9
Description: Potent P2Y12 antagonist; orally available
Chemical Name: 5-Chloro-N-[6-[5-methyl-4-(1-oxobutyl)-1H-pyrazol-1-yl]-3-pyridazinyl]-1-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-1H-indole-3-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent P2Y12 antagonist (IC50 = 17 nM). Displays antiplatelet and antithrombotic activity in vivo. Orally available.

Technical Data

M. Wt 599.51
Formula C28H31ClN8O3.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1279829-64-9
PubChem ID 70926954
InChI Key UQLWHBMSQKUYAI-UHFFFAOYSA-N
Smiles ClC1=CC=C2C(C(C(NC3=CC=C(N4C(C)=C(C(CCC)=O)C=N4)N=N3)=O)=CN2CC(N5CCN(C)CC5)=O)=C1.Cl

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.99 20mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 599.51. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 1.67 mL 8.34 mL 16.68 mL
5 mM 0.33 mL 1.67 mL 3.34 mL
10 mM 0.17 mL 0.83 mL 1.67 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Boldron et al (2014) N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist. J.Med.Chem. 57 7293 PMID: 25075638


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Keywords: SAR216471 hydrochloride potent P2Y12 antagonists antiplatelets antithrombotics orally available bioavailable purine receptors purinoceptors purinergic Purinergic P2Y Receptors

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