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

BMS-986020 sodium  (Synonyms: AM152 sodium)

Cat. No.: HY-100619A Purity: 99.41%
SDS COA Handling Instructions

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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 (AM152) 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

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10 mM * 1 mL in DMSO
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Based on 7 publication(s) in Google Scholar

Other Forms of BMS-986020 sodium:

BMS-986020 sodium Related Antibodies

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Description

BMS-986020 (AM152) 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].

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

BMS-986020 sodium Related Antibodies
Clinical Trial
Molecular Weight

504.51

Formula

C29H25N2NaO5
CAS No.
Appearance

Solid

Color

Light yellow 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[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; 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 1.9821 mL 9.9106 mL 19.8212 mL
5 mM 0.3964 mL 1.9821 mL 3.9642 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 7.5 mg/mL (14.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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% (20% SBE-β-CD in Saline)

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

    This protocol yields a suspended solution of 7.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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:  50% PEG300    50% Saline

    Solubility: 25 mg/mL (49.55 mM); Clear 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).

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

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: 99.41%

SDS (393 KB)

COA (259 KB) LCMS (100 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9821 mL 9.9106 mL 19.8212 mL 49.5530 mL
5 mM 0.3964 mL 1.9821 mL 3.9642 mL 9.9106 mL
10 mM 0.1982 mL 0.9911 mL 1.9821 mL 4.9553 mL
15 mM 0.1321 mL 0.6607 mL 1.3214 mL 3.3035 mL
20 mM 0.0991 mL 0.4955 mL 0.9911 mL 2.4777 mL
25 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9821 mL
30 mM 0.0661 mL 0.3304 mL 0.6607 mL 1.6518 mL
40 mM 0.0496 mL 0.2478 mL 0.4955 mL 1.2388 mL
50 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9911 mL
60 mM 0.0330 mL 0.1652 mL 0.3304 mL 0.8259 mL
80 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6194 mL
100 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4955 mL
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BMS-986020 sodium 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-9860201380650-53-2AM152BMS986020BMS 986020AM 152AM-152LPL ReceptorLysophospholipid ReceptoridiopathicpulmonaryfibrosisIPFautoradiographyARGInhibitorinhibitorinhibit

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