2. GPCR/G Protein Apoptosis Metabolic Enzyme/Protease
  3. Adenosine Receptor Apoptosis PGC-1α
  4. LJ-2698

LJ-2698 is an orally active adenosine A3 receptor antagonist. LJ-2698 induces increased levels of anti-inflammatory cytokines in macrophages and significantly elevates the number of anti-inflammatory M2 macrophages in the lung. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, inhibits matrix metalloproteinase activity and pulmonary cell apoptosis in the lung tissues of mice. LJ-2698 prevents renal injury, inhibits renal lipid accumulation, and increases PGC1α levels in renal tissues of mice with diabetic nephropathy. LJ-2698 is applicable to the research of emphysema and diabetic nephropathy.

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

LJ-2698

LJ-2698 Chemical Structure

CAS No. : 945457-84-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

LJ-2698 Related Antibodies

Top Publications Citing Use of Products

View All Adenosine Receptor Isoform Specific Products:

View All Isoforms
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LJ-2698 is an orally active adenosine A3 receptor antagonist. LJ-2698 induces increased levels of anti-inflammatory cytokines in macrophages and significantly elevates the number of anti-inflammatory M2 macrophages in the lung. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, inhibits matrix metalloproteinase activity and pulmonary cell apoptosis in the lung tissues of mice. LJ-2698 prevents renal injury, inhibits renal lipid accumulation, and increases PGC1α levels in renal tissues of mice with diabetic nephropathy. LJ-2698 is applicable to the research of emphysema and diabetic nephropathy[1][2].

In Vitro

LJ-2698 (0.1 μM, 72 h) restores the expression of anti-inflammatory cytokines (Il4, Il10) and M2 macrophage markers (Arg1, Mrc1) in LPS-stimulated RAW 264.7 mouse macrophages[1].

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

LJ-2698 Related Antibodies

Real Time qPCR[1]

Cell Line: RAW 264.7 (murine macrophage)
Concentration: 0.1 μM
Incubation Time: 48 h (pretreatment); 24 h (co-incubation with LPS)
Result: Significantly ameliorated LPS-mediated downregulation of Il4 and Il10 anti-inflammatory cytokine mRNA expression.
Significantly restored LPS-mediated downregulation of Arg1 and Mrc1 M2 macrophage marker mRNA expression.
In Vivo

LJ-2698 (50 μg/kg; p.o.; 6 times per week for 5 consecutive weeks) significantly inhibits Elastase, Porcine pancreas (HY-P2974)-induced emphysema in FVB mice by restoring pulmonary function, reducing airspace enlargement, inhibiting matrix metalloproteinase activity and pulmonary cell apoptosis, and promoting M2 macrophage-mediated anti-inflammatory responses, with extremely low observed toxicity[1].
LJ-2698 (1.5-10 mg/kg; p.o.; once daily; for 12 weeks) improves diabetic nephropathy in db/db mice in a dose-dependent manner, and the 10 mg/kg dose exhibits the most stable and comprehensive renoprotective effects across all detected indicators[2].

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

Animal Model: FVB mice (8-week-old)[1]
Dosage: 50 μg/kg
Administration: p.o.; 6 times per week; 5 weeks
Result: Restored lung compliance and tissue elasticity to levels closer to control mice.
Markedly suppressed PPE-induced airspace enlargement and reduced the elevated PPE-induced mean linear intercept (MLI).
Suppressed PPE-mediated increases in matrix metalloproteinase gelatinase activity in lung tissue.
Significantly reduced the number of TUNEL-positive apoptotic cells in the lungs compared to PPE-only treated mice.
Restored PPE-induced downregulation of anti-inflammatory cytokine (Il4, Il10) and M2 macrophage marker (Arg1, Mrc1/CD206) mRNA expression in lung tissue.
Increased the number of CD206-positive M2 macrophages per field in lung tissue.
Caused no significant changes in body weight compared to control or PPE-only groups, indicating minimal toxicity.
Animal Model: C57BLKS/J-db/db (male, 8 weeks old)[2]
Dosage: 1.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 12 weeks
Result: Significantly reduced elevated glomerular volume and fractional mesangial area across all three doses, with no significant differences between doses.
Significantly reduced increased urinary albumin excretion at 5 and 10 mg/kg doses; did not produce a significant reduction at 1.5 mg/kg dose.
Significantly prevented reduced nephrin mRNA levels and increased NGAL mRNA levels at 10 mg/kg dose.
Significantly inhibited increased TGF-β mRNA levels at 10 mg/kg dose; did not produce a significant reduction at 1.5 and 5 mg/kg doses.
Significantly reduced increased collagen IV and fibronectin mRNA levels at 5 and 10 mg/kg doses.
Significantly reduced elevated MCP-1 mRNA levels at 5 and 10 mg/kg doses; significantly inhibited increased ICAM-1 mRNA levels at 10 mg/kg dose, while 1.5 and 5 mg/kg doses did not.
Significantly decreased increased urinary LPO levels at 5 and 10 mg/kg doses.
Molecular Weight

412.29

Formula

C16H15Cl2N5O2S
CAS No.
SMILES

N(CC1=CC(Cl)=CC=C1)C2=C3C(N(C=N3)[C@H]4[C@H](O)[C@H](O)CS4)=NC(Cl)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

LJ-2698 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

LJ-2698945457-84-1LJ2698LJ 2698Adenosine ReceptorApoptosisPGC-1αP1 receptorPPARγ coactivator-1αpulmonary emphysemaFVB miceadenosine A3 receptormacrophagesRAW 264.7 murine macrophage cellsdiabetic kidney diseaseM2 macrophagemurine lung tissueMLE-12db/db mouseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LJ-2698
Cat. No.:
HY-153149
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.