ML-354
IC50: 140 nM
ML-354 is an indole-based, proteinase-activated receptor (PAR) 4 antagonist with good potency and reasonable selectivity versus PAR1. PARs are a family of four G-protein-coupled receptors GPCRs (PAR1-PAR4) with several unique attributes, which are activated by serine proteases. The activation of PARs needs a unique mechanism which requiring proteolysis unmasking their extracellular N-terminal domain. PAR4 is a thrombin receptor found on human platelets and represents a potential therapeutic target for the treatment of thrombotic disorders [1].
In vitro: Up to now, in vitro study of ML-354 is still in the development stage.
In vivo: Up to now, in vivo study of ML-354 is still in the development stage.
Reference:
[1]. Wen, W., Young, S., Duvernay, M., Schulte, M., Nance, K., & Melancon, B. et al. Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorganic & Medicinal Chemistry Letters. 2014; 24(19): 4708-4713.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 282.3 |
| Cas No. | 89159-60-4 |
| Formula | C16H14N2O3 |
| Synonyms | VU0099704 |
| Solubility | ≤2mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | 1-methyl-5-nitro-3-phenyl-1H-indole-2-methanol |
| SDF | Download SDF |
| Canonical SMILES | CN1C(CO)=C(C2=CC=CC=C2)C3=C1C=CC([N+]([O-])=O)=C3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
