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BMS-986278 - 99%, high purity , CAS No.2170126-74-4

COA COA
In stock
Item Number
B648666
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B648666-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$179.90
B648666-25mg
25mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$463.90
B648666-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$614.90
B648666-100mg
100mg
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$907.90
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Bulk Order  SDS  DATASHEET  Specification Sheet
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Class A GPCR (4138) GPCR/G Protein (3172) LPL Receptor (113)

Basic Description

Specifications & Purity Moligand™, ≥99%
Biochemical and Physiological Mechanisms BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Product Description

BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases

In Vitro

BMS-986278 is a high-affinity LPA1 antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1. BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a K b of 5.8 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BMS-986278 (0.1-10 mg/kg; a single p.o.) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner in CD1 mice . BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats . Pharmacokinetics of BMS-986278 in preclinical species plasma clearance ((mL/min)/kg) V ss (L/kg) oral bioavailability (%) T 1/2 (h) plasma protein binding (% free) mouse 37 5.5 70 2.5 31.4 rat 15 3.5 100 4.5 12.6 monkey 2.0 1.6 79 11 0.8 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (10 weeks) were administered Bleomycin Dosage: 3, 10, and 30 mg/kg Administration: P.o. twice daily for 14 days Result: Resulted in significant decreases in the lung section percent fibrotic area for the 3 mg/kg (48%) and 10 mg/kg (56%) dose groups.

Form:Solid

IC50& Target:Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)

Associated Targets(Human)

KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LPAR1 Tchem Lysophosphatidic acid receptor Edg-2 (779 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCB11 Tchem Bile salt export pump (2311 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC3 Tbio Canalicular multispecific organic anion transporter 2 (718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC4 Tchem Multidrug resistance-associated protein 4 (785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCB4 Tbio Multidrug resistance protein 3 (8 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Smiles CCCN(C)C(=O)OCC1=C(N=NN1C)C2=NC(=C(C=C2)O[C@H]3CCC[C@@H](C3)C(=O)O)C
Isomeric SMILES CCCN(C)C(=O)OCC1=C(N=NN1C)C2=NC(=C(C=C2)O[C@H]3CCC[C@@H](C3)C(=O)O)C
PubChem CID 132232205
Molecular Weight 445.51

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 100 mg/mL (224.46 mM; Need ultrasonic)
Molecular Weight 445.500 g/mol
XLogP3 2.100
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 9
Exact Mass 445.233 Da
Monoisotopic Mass 445.233 Da
Topological Polar Surface Area 120.000 Ų
Heavy Atom Count 32
Formal Charge 0
Complexity 638.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 2
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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