Lu-135252 - 98%, high purity , Endothelin receptor ET-B antagonist, CAS No.171714-84-4, Endothelin receptor ET-B antagonist

Item Number
L412123
Grouped product items
SKUSizeAvailabilityPrice Qty
L412123-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$29.90
L412123-5mg
5mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$99.90
L412123-10mg
10mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$159.90
L412123-25mg
25mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$299.90
L412123-50mg
50mg
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$499.90
L412123-100mg
100mg
Available within 8-12 weeks(?)
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$729.90
View related series
ETA receptor Antagonist

Basic Description

SynonymsLU135252 | 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-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsLu-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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionEndothelin 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.

Product Properties

ALogP3.6

Associated Targets(Human)

EDNRA Tclin Endothelin-1 receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EDNRB Tclin Endothelin receptor type B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EDNRB Tclin Endothelin receptor ET-B (1928 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EDNRB Tclin Endothelin receptor, ET-A/ET-B (286 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Ednra Endothelin receptor (172 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
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

Certificates

Certificate of Analysis(COA)

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12 results found

Lot NumberCertificate TypeDateItem
B2418413Certificate of AnalysisJan 04, 2024 L412123
B2418414Certificate of AnalysisJan 04, 2024 L412123
B2418415Certificate of AnalysisJan 04, 2024 L412123
B2418416Certificate of AnalysisJan 04, 2024 L412123
B2418417Certificate of AnalysisJan 04, 2024 L412123
B2418418Certificate of AnalysisJan 04, 2024 L412123
B2418419Certificate of AnalysisJan 04, 2024 L412123
B2418420Certificate of AnalysisJan 04, 2024 L412123
B2418421Certificate of AnalysisJan 04, 2024 L412123
B2418422Certificate of AnalysisJan 04, 2024 L412123
B2418424Certificate of AnalysisJan 04, 2024 L412123
B2418425Certificate of AnalysisJan 04, 2024 L412123

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Safety and Hazards(GHS)

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.

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