2. GPCR/G Protein Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  3. CCR Histamine Receptor Calcium Channel
  4. YM-344484

YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis.

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

YM-344484

YM-344484 Chemical Structure

CAS No. : 671205-14-4

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.

YM-344484 Related Antibodies

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

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

View All Histamine Receptor Isoform Specific Products:

View All Isoforms
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

View All Calcium Channel Isoform Specific Products:

View All Isoforms
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis[1].

IC50 & Target[1]

CCR3

 

H1 Receptor

 

In Vitro

YM-344484 potently inhibits CCR3 ligand-induced calcium influx in B300-19 cells expressing human CCR3, with its Kβ values ranging from 0.69 nM to 2.5 nM depending on the ligand[1].
YM-344484 inhibits CCL11-induced calcium influx in mouse CCR3-expressing cells, with a Kβ value of 88 nM[1].
YM-344484 inhibits histamine H1 receptor-mediated calcium influx in PC3 cells, with a Kβ value of 47 nM[1].
YM-344484 (10 μM) exhibits only weak inhibitory activity against serotonin 5-HT2A receptor-mediated calcium influx in C6 cells, with an inhibition rate of merely 25%[1].
YM-344484 potently inhibits CCR3 ligand-induced chemotaxis in human CCR3-expressing B300-19 cells, with its IC50 values ranging from 2.0 nM to 8.0 nM depending on the ligand[1].
YM-344484 inhibits the release of eosinophil-derived neurotoxin from human peripheral blood eosinophils induced by CCL11, with an IC50 value of 19 nM[1].

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

YM-344484 Related Antibodies
In Vivo

YM-344484 (3-30 mg/kg; p.o.; single administration) achieves an 82% inhibition rate of Histamine (HY-B1204)-induced vascular permeability in mice at a single oral dose of 10 mg/kg, and complete inhibition is attained at the 30 mg/kg dose[1].
YM-344484 (100-600 mg/kg; p.o.; once every 8 hours; 6 doses total) inhibits eosinophil infiltration by 74% at the dose of 300 mg/kg, and completely suppresses eosinophil infiltration at the dose of 600 mg/kg, in a mouse asthma model induced by Ovalbumins (HY-W250978)[1].

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

Animal Model: Balb/c (female, 6 weeks old)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Suppressed histamine-induced vascular permeability dose-dependently.
Achieved statistically significant 82% inhibition at 10 mg/kg.
Achieved complete inhibition at 30 mg/kg.
Animal Model: Balb/c (female)[1]
Dosage: 100 mg/kg; 300 mg/kg; 600 mg/kg
Administration: p.o.; every 8 hours; 6 doses
Result: Failed to reduce eosinophil numbers at 100 mg/kg.
Significantly attenuated eosinophil infiltration with 74% inhibition at 300 mg/kg.
Achieved 100% inhibition of eosinophil infiltration at 600 mg/kg.
Exhibited no inhibitory effect on neutrophil or mononuclear cell counts in bronchoalveolar lavage fluid.
Molecular Weight

487.57

Formula

C28H30FN5O2
CAS No.
SMILES

FC(C=C1)=CC(C=C2)=C1C=C2CN3C[C@@H](CC3)NC(/C=C4CCN(CC/4)C(C5=CC=C(N=N5)C)=O)=O
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.

YM-344484 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:

YM-344484671205-14-4YM344484YM 344484CCRHistamine ReceptorCalcium ChannelCC chemokine receptorCa2+ channelsCa channelshuman peripheral blood eosinophilshistamine H1 receptorallergic rhinitisC6 cellsatopic dermatitisCCR3 receptorG-protein-coupled receptorsasthmaB300-19 cellsPC3 cellsInhibitorinhibitorinhibit

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:
YM-344484
Cat. No.:
HY-182736
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.