2. GPCR/G Protein
  3. LPL Receptor
  4. BMS-986278

BMS-986278 

Cat. No.: HY-139853 Purity: 99.60%
COA Handling Instructions

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs 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.

For research use only. We do not sell to patients.

BMS-986278 Chemical Structure

BMS-986278 Chemical Structure

CAS No. : 2170126-74-4

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10 mg USD 1120 In-stock
25 mg USD 2250 In-stock
50 mg USD 3650 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs 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[1].

IC50 & Target

Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)[1]
In Vitro

BMS-986278 is a high-affinity LPA1 antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1[1].
BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a Kb of 5.8 nM[1].

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[1].
BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats[1].

Pharmacokinetics of BMS-986278 in preclinical species[1]

plasma clearance ((mL/min)/kg) Vss (L/kg) oral bioavailability (%) T1/2 (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[1]
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.
Clinical Trial
Molecular Weight

445.51

Appearance

Solid

Formula

C22H31N5O5
CAS No.
SMILES

CCCN(C)C(OCC1=C(N=NN1C)C(C=C2)=NC(C)=C2O[[email protected]]3CCC[[email protected]](C(O)=O)C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (224.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2446 mL 11.2231 mL 22.4462 mL
5 mM 0.4489 mL 2.2446 mL 4.4892 mL
10 mM 0.2245 mL 1.1223 mL 2.2446 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.60%

COA (255 KB) HNMR (205 KB) LCMS (128 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

BMS-9862782170126-74-4BMS986278BMS 986278LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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