2. GPCR/G Protein
  3. LPL Receptor
  4. BMS-986020

BMS-986020 est un antagoniste des récepteurs de l'acide lysophosphatidique 1 (LPA1) de haute affinité et sélectif. BMS-986020 inhibe les transporteurs d'acide biliaire et de phospholipides avec des IC50s de 4,8 µM, 6,2 µM et 7,5 µM pour BSEP, MRP4 et MDR3, respectivement[ 2]. BMS-986020 a le potentiel pour le traitement de la fibrose pulmonaire idiopathique (IPF).

BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 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 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

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

BMS-986020 Chemical Structure

BMS-986020 Chemical Structure

CAS No. : 1257213-50-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 101 In-stock
Solution
10 mM * 1 mL in DMSO USD 101 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 95 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of BMS-986020:

BMS-986020 Related Antibodies

Top Publications Citing Use of Products

View All LPL Receptor Isoform Specific Products:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist[1]. BMS-986020 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 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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986020 Related Antibodies
Clinical Trial
Molecular Weight

482.53

Formula

C29H26N2O5
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

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

DMSO : 125 mg/mL (259.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0724 mL 10.3621 mL 20.7241 mL
5 mM 0.4145 mL 2.0724 mL 4.1448 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 5 mg/mL (10.36 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

SDS (393 KB)

COA (259 KB) HNMR (270 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0724 mL 10.3621 mL 20.7241 mL 51.8103 mL
5 mM 0.4145 mL 2.0724 mL 4.1448 mL 10.3621 mL
10 mM 0.2072 mL 1.0362 mL 2.0724 mL 5.1810 mL
15 mM 0.1382 mL 0.6908 mL 1.3816 mL 3.4540 mL
20 mM 0.1036 mL 0.5181 mL 1.0362 mL 2.5905 mL
25 mM 0.0829 mL 0.4145 mL 0.8290 mL 2.0724 mL
30 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7270 mL
40 mM 0.0518 mL 0.2591 mL 0.5181 mL 1.2953 mL
50 mM 0.0414 mL 0.2072 mL 0.4145 mL 1.0362 mL
60 mM 0.0345 mL 0.1727 mL 0.3454 mL 0.8635 mL
80 mM 0.0259 mL 0.1295 mL 0.2591 mL 0.6476 mL
100 mM 0.0207 mL 0.1036 mL 0.2072 mL 0.5181 mL
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BMS-986020 Related Classifications

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.

Keywords:

BMS-9860201257213-50-5AM152BMS986020BMS 986020AM 152AM-152LPL ReceptorLysophospholipid ReceptoridiopathicpulmonaryfibrosisIPFautoradiographyARGInhibitorinhibitorinhibit

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