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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S413561-5mg | 5mg | In stock | $197.90 | |
S413561-10mg | 10mg | In stock | $315.90 | |
S413561-25mg | 25mg | In stock | $459.90 | |
S413561-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $711.90 | |
S413561-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $890.90 |
TRP Channel Inhibitors
Specifications & Purity | Moligand™, ≥97% |
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Biochemical and Physiological Mechanisms | SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of TRPC3;Channel blocker of TRPC6;Channel blocker of TRPC7 |
Product Description | Information SAR7334 SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. Targets TPRC6 (Cell-free assay) 7.9nM In vitro SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected..SAR7334 suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice. In vivo Pharmacokinetic studies of SAR7334 demonstrates that the compound was suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR). Cell Research(from reference) Cell lines:HEK cells |
ALogP | 3.871 |
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HBD Count | 1 |
Rotatable Bond | 3 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[[(1R,2R)-2-[(3R)-3-aminopiperidin-1-yl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chlorobenzonitrile |
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INCHI | InChI=1S/C21H22ClN3O/c22-18-10-14(12-23)7-8-20(18)26-21-17-6-2-1-4-15(17)11-19(21)25-9-3-5-16(24)13-25/h1-2,4,6-8,10,16,19,21H,3,5,9,11,13,24H2/t16-,19-,21-/m1/s1 |
InChi Key | RLKRLNQEXBPQGQ-OZOXKJRCSA-N |
Canonical SMILES | C1CC(CN(C1)C2CC3=CC=CC=C3C2OC4=C(C=C(C=C4)C#N)Cl)N |
Isomeric SMILES | C1C[C@H](CN(C1)[C@@H]2CC3=CC=CC=C3[C@H]2OC4=C(C=C(C=C4)C#N)Cl)N |
PubChem CID | 53378752 |
Molecular Weight | 367.87 |
PubChem CID | 53378752 |
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CAS Registry No. | 1333210-07-3 |
RCSB PDB Ligand | HOR |
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Solubility | Solubility (25°C) In vitro DMSO: 74 mg/mL (201.15 mM); Ethanol: 74 mg/mL (201.15 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 74 |
DMSO(mM) Max Solubility | 201.158017778019 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Maier T, Follmann M, Hessler G, Kleemann HW, Hachtel S, Fuchs B, Weissmann N, Linz W, Schmidt T, Löhn M et al.. (2015) Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels.. Br J Pharmacol, 172 (14): (3650-60). [PMID:25847402] [10.1021/op500134e] |