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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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L412123-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $29.90 | |
L412123-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $99.90 | |
L412123-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $159.90 | |
L412123-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $299.90 | |
L412123-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $499.90 | |
L412123-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $729.90 |
Synonyms | LU135252 | LU-135252 | Darusentan [INN] | GTPL3508 | BCP13024 | WGA71484 | Benzenepropanoic acid, alpha-((4,6-dimethoxy-2-pyrimidinyl)oxy)-beta-methoxy-beta-phenyl-, (S)- | BDBM50108202 | Darusentan | 3-(8,8-diethyl-3-aza-8-germaspiro[4.5]decan-3-yl)-N,N- |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Lu-135252 (Darusentan, HMR-4005) is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics with Ki of 13 nM. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Endothelin receptor ET-B antagonist |
Product Description | Information Lu-135252 (Darusentan, HMR-4005) is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics with Ki of 13 nM. |
ALogP | 3.6 |
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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 | (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid |
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INCHI | InChI=1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1 |
InChi Key | FEJVSJIALLTFRP-LJQANCHMSA-N |
Canonical SMILES | COC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC |
Isomeric SMILES | COC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC |
PubChem CID | 177236 |
Molecular Weight | 410.43 |
Wikipedia | Darusentan |
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CAS Registry No. | 171714-84-4 |
PubChem CID | 177236 |
ChEMBL Ligand | CHEMBL23261 |
GPCRdb Ligand | darusentan |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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B2418413 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418414 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418415 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418416 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418417 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418418 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418419 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418420 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418421 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418422 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418424 | Certificate of Analysis | Jan 04, 2024 | L412123 |
B2418425 | Certificate of Analysis | Jan 04, 2024 | L412123 |
Signal | Warning |
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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. |