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BMS-986020 - 99%, high purity , Lysophosphatidic acid receptor Edg-2 antagonist, CAS No.1257213-50-5, Lysophosphatidic acid receptor Edg-2 antagonist

Moligand™
≥99%

CAS#: 1257213-50-5
Formula: C₂₉H₂₆N₂O₅
Molecular Weight: 482.53
PubChem CID: 49792850
PubChem SID: 488201431

Item Number

B413030

Grouped product items
SKU	Size	Availability	Price
B413030-5mg	5mg	In stock	$93.90
B413030-10mg	10mg	In stock	$147.90
B413030-25mg	25mg	In stock	$333.90
B413030-50mg	50mg	In stock	$444.90
B413030-100mg	100mg	In stock	$741.90

LPA Receptor Antagonists

View related series

LPA1 receptor Antagonist

Basic Description

Synonyms	BMS-986020\|1257213-50-5\|AP-3152 free acid\|Cyclopropanecarboxylic acid, 1-[4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl][1,1'-biphenyl]-4-yl]-\|BMS 986020\|38CTP01B4L\|(R)-1-(4'-(3-Methyl-4-(((1-phenylethoxy)carbonyl)amino)isoxazol-5-yl)
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respective
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Lysophosphatidic acid receptor Edg-2 antagonist
Product Description	Information BMS-986020 BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1) . BMS-986020 inhibits bile acid and phospholipid transporters with IC50 of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF). Targets LPA1 ; BSEP (Cell-free assay); MRP4 (Cell-free assay); MDR3 (Cell-free assay) ; 4.8 μM; 6.2 μM; 7.5 μM

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

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CYP2C8 Tchem Cytochrome P450 2C8 0 Activities

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CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

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CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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CYP2B6 Tchem Cytochrome P450 2B6 0 Activities

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CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

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ABCB4 Tbio Phosphatidylcholine translocator ABCB4 0 Activities

Discover Target: ABCB4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 0 Activities

Discover Target: SLCO1B1

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SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 0 Activities

Discover Target: SLCO1B3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LPAR1 Tchem Lysophosphatidic acid receptor 1 1 Activities

Discover Target: LPAR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCC3 Tbio Canalicular multispecific organic anion transporter 2 0 Activities

Discover Target: ABCC3

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ABCC4 Tchem Multidrug resistance-associated protein 4 0 Activities

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ABCB11 Tchem Bile salt export pump 0 Activities

Discover Target: ABCB11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Pubchem Sid	488201431
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/488201431
IUPAC Name	1-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
INCHI	InChI=1S/C29H26N2O5/c1-18-25(30-28(34)35-19(2)20-6-4-3-5-7-20)26(36-31-18)23-10-8-21(9-11-23)22-12-14-24(15-13-22)29(16-17-29)27(32)33/h3-15,19H,16-17H2,1-2H3,(H,30,34)(H,32,33)/t19-/m1/s1
InChi Key	GQBRZBHEPUQRPL-LJQANCHMSA-N
Canonical SMILES	CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5(CC5)C(=O)O
Isomeric SMILES	CC1=NOC(=C1NC(=O)O[C@H](C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5(CC5)C(=O)O
PubChem CID	49792850
Molecular Weight	482.53

PubChem CID

CAS Registry No.

GPCRdb Ligand

PubChem SID

Certificates

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10 results found

Lot Number	Certificate Type	Date	Item
C2323320	Certificate of Analysis	Feb 03, 2023	B413030
C2323323	Certificate of Analysis	Feb 03, 2023	B413030
C2323327	Certificate of Analysis	Feb 03, 2023	B413030
C2323348	Certificate of Analysis	Feb 03, 2023	B413030
C2323377	Certificate of Analysis	Feb 03, 2023	B413030
C2323384	Certificate of Analysis	Feb 03, 2023	B413030
C2323450	Certificate of Analysis	Feb 03, 2023	B413030
C2323462	Certificate of Analysis	Feb 03, 2023	B413030
C2323763	Certificate of Analysis	Feb 03, 2023	B413030
C2323989	Certificate of Analysis	Feb 03, 2023	B413030

References

1. Kihara Y, Mizuno H, Chun J. (2015) Lysophospholipid receptors in drug discovery.. Exp Cell Res, 333 (2): (171-7). [PMID:25499971]
2. Palmer SM, Snyder L, Todd JL, Soule B, Christian R, Anstrom K, Luo Y, Gagnon R, Rosen G. (2018) Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis.. Chest, 154 (5): (1061-1069). [PMID:30201408]

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