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  3. BMS-986020 sodium

BMS-986020 sodium 

Cat. No.: HY-100619A Purity: 99.60%
Handling Instructions

BMS-986020 sodium est un antagoniste du récepteur 1 de l'acide lysophosphatidique de haute affinité(LPA1). BMS-986020 sodium inhibe les transporteurs d'acide biliaire et de phospholipides avec des IC50 de 4,8 µM, 6,2 µM et 7,5 µM pour BSEP, MRP4 et MDR3, respectivement. BMS-986020 sodium a le potentiel pour le traitement de la fibrose pulmonaire idiopathique (IPF).

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

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

BMS-986020 sodium Chemical Structure

BMS-986020 sodium Chemical Structure

CAS No. : 1380650-53-2

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 105 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist[1]. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively[2]. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF)[3].

IC50 & Target

IC50: 4.8 µM (BSEP); 6.2 µM (MRP4); 7.5 µM (MDR3)[2]

In Vitro

BMS-986020 sodium (0.1-10 nM; pre-incubated) concentration-dependent displacement of [18F]BMT-083133 binding is observed in LPA1+ cells and lung sections. At 0.1 nM, the percent displacement in healthy mice, bleomycin mice, and IPF lungs is 18%, 24%, and 31%, respectively. At 10 nM, the percent displacement is 73%, 76%, and 64%, respectively.
[18F]BMT-083133, a radioligand targeting LPA1 is developed as a translational research tool for assessment of lung LPA1 engagement of BMS-986020 using in vitro autoradiography (ARG)[4].

Clinical Trial
Molecular Weight

504.51

Formula

C₂₉H₂₅N₂NaO₅

CAS No.

1380650-53-2

SMILES

O=C(C1(C2=CC=C(C3=CC=C(C4=C(NC(O[[email protected]@H](C5=CC=CC=C5)C)=O)C(C)=NO4)C=C3)C=C2)CC1)O[Na]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (297.32 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9821 mL 9.9106 mL 19.8212 mL
5 mM 0.3964 mL 1.9821 mL 3.9642 mL
10 mM 0.1982 mL 0.9911 mL 1.9821 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: ≥ 7.5 mg/mL (14.87 mM); Clear solution

  • 2.

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

    Solubility: 7.5 mg/mL (14.87 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Suspended solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.60%

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Keywords:

BMS-986020BMS986020BMS 986020LPL ReceptorLysophospholipid ReceptoridiopathicpulmonaryfibrosisIPFautoradiographyARGInhibitorinhibitorinhibit

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Product name:
BMS-986020 sodium
Cat. No.:
HY-100619A
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