2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. BMS-813160

BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation.

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

BMS-813160 Chemical Structure

BMS-813160 Chemical Structure

CAS No. : 1286279-29-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 181 In-stock
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10 mM * 1 mL in DMSO USD 181 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BMS-813160 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BMS-813160

View All CCR Isoform Specific Products:

View All Isoforms
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation[1][2].

IC50 & Target[1]

CCR5

3.6 nM (IC50)

CCR2

6.2 nM (IC50)

In Vitro

BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively[2].
BMS-813160 shows activities to CCR2 CTX, CCR2 CD11b, CCR5 CTX and CCR5 CD11b with IC50s of 0.8, 4.8, 1.1 and 5.7 nM, respectively[2].

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

BMS-813160 Related Antibodies
In Vivo

BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability[2].

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

Animal Model: Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injection[2]
Dosage: 10, 50 and 160 mg/kg
Administration: Oral gavage; 10-160 mg/kg twice a day; for two days
Result: Dose-dependently reduced inflammatory monocyte and macrophage infiltration in the peritoneum.
Clinical Trial
Molecular Weight

484.64

Formula

C25H40N8O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N[C@H]1[C@@H](N2C([C@@H](NC3=NC=NC4=CC(C(C)(C)C)=NN43)CC2)=O)CC[C@@H](NC(C)(C)C)C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (206.34 mM; Need ultrasonic)

DMSO : 25 mg/mL (51.58 mM; Need ultrasonic and warming; 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 2.0634 mL 10.3169 mL 20.6339 mL
5 mM 0.4127 mL 2.0634 mL 4.1268 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • 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: ≥ 2.08 mg/mL (4.29 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.29 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 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.
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 (protect from light)

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: 99.93%

SDS (581 KB)

COA (257 KB) HNMR (263 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, 6 months; -20°C, 1 month (protect from light). 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 / Ethanol 1 mM 2.0634 mL 10.3169 mL 20.6339 mL 51.5847 mL
5 mM 0.4127 mL 2.0634 mL 4.1268 mL 10.3169 mL
10 mM 0.2063 mL 1.0317 mL 2.0634 mL 5.1585 mL
15 mM 0.1376 mL 0.6878 mL 1.3756 mL 3.4390 mL
20 mM 0.1032 mL 0.5158 mL 1.0317 mL 2.5792 mL
25 mM 0.0825 mL 0.4127 mL 0.8254 mL 2.0634 mL
30 mM 0.0688 mL 0.3439 mL 0.6878 mL 1.7195 mL
40 mM 0.0516 mL 0.2579 mL 0.5158 mL 1.2896 mL
50 mM 0.0413 mL 0.2063 mL 0.4127 mL 1.0317 mL
Ethanol 60 mM 0.0344 mL 0.1719 mL 0.3439 mL 0.8597 mL
80 mM 0.0258 mL 0.1290 mL 0.2579 mL 0.6448 mL
100 mM 0.0206 mL 0.1032 mL 0.2063 mL 0.5158 mL
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BMS-813160 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-8131601286279-29-5BMS813160BMS 813160CCRCC chemokine receptordual antagonistCD11bCTXthioglycollateperitonitismouseoralinflammationInhibitorinhibitorinhibit

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