2. GPCR/G Protein
  3. LPL Receptor
  4. AMG 369

AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat.

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

AMG 369

AMG 369 Chemical Structure

CAS No. : 1202073-26-4

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.

AMG 369 Related Antibodies

Top Publications Citing Use of Products

View All LPL Receptor Isoform Specific Products:

View All Isoforms
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat[1].

IC50 & Target[1]

S1PR1

 

S1PR5

 

S1PR3

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.029 μM
Compound: 5d, AMG-369
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
[PMID: 24900288]
CHO EC50
0.888 μM
Compound: 5d, AMG-369
Agonist activity at human S1P3R expressed in CHO cells by Ca(2+) mobilization assay
Agonist activity at human S1P3R expressed in CHO cells by Ca(2+) mobilization assay
[PMID: 24900288]
CHO EC50
0.888 μM
Compound: AMG-369
Agonist activity at human S1P3 receptor expressed in CHO cells coexpressing Gq/i5 protein by calcium flux assay
Agonist activity at human S1P3 receptor expressed in CHO cells coexpressing Gq/i5 protein by calcium flux assay
[PMID: 22100314]
CHO EC50
0.888 μM
Compound: AMG-369
Agonist activity at human S1P3 receptor expressed in CHO cells coexpressing chimeric Gq/i5 G-protein assessed as Ca2+ release by FLIPR assay
Agonist activity at human S1P3 receptor expressed in CHO cells coexpressing chimeric Gq/i5 G-protein assessed as Ca2+ release by FLIPR assay
[PMID: 22257889]
U2OS EC50
0.002 μM
Compound: 5d, AMG-369
Induction of human GFP-tagged chimeric S1P1R internalization in human U2Os cells by fluorescence microscopy
Induction of human GFP-tagged chimeric S1P1R internalization in human U2Os cells by fluorescence microscopy
[PMID: 24900288]
U2OS EC50
0.002 μM
Compound: AMG-369
Agonist activity at human S1P1 receptor expressed in U20S cells coexpressing eGFP assessed as receptor internalization after 1 hr by microscopy analysis
Agonist activity at human S1P1 receptor expressed in U20S cells coexpressing eGFP assessed as receptor internalization after 1 hr by microscopy analysis
[PMID: 22100314]
U2OS EC50
0.002 μM
Compound: AMG-369
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
[PMID: 22257889]
In Vitro

AMG 369 potently induces internalization of hS1P1-GFP fusion protein in U2OS cells with an EC50 of 0.002 μM and 98% efficacy[1].
AMG 369 weakly induces Ca2+ mobilization via hS1P3 in transfected CHO-K1 cells with an EC50 of 0.888 μM and 26% efficacy[1].

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

AMG 369 Related Antibodies
In Vivo

AMG 369 (0.01-0.1 mg/kg; p.o.; single dose) produces dose-dependent, statistically significant reductions in blood lymphocyte counts at 0.03 mg/kg (45% reduction) and 0.1 mg/kg (65% reduction) 24 hours postdose in female Lewis rats [1].
AMG 369 (0.1 mg/kg; p.o.; single dose) delays the onset and reduces clinical disease severity in a female Lewis rat experimental autoimmune encephalomyelitis model[1].

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

Animal Model: Lewis rats (female)[1]
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg
Administration: p.o.; single dose
Result: Produced a non-statistically significant reduction in blood lymphocytes at 0.01 mg/kg vs vehicle.
Produced a statistically significant 45% reduction in blood lymphocytes at 0.03 mg/kg vs vehicle.
Produced a statistically significant 65% reduction in blood lymphocytes at 0.1 mg/kg vs vehicle, nearly the maximal 70% reduction typically observed with S1P1 agonists.
Animal Model: Lewis rats (female; experimental autoimmune encephalomyelitis model induced by guinea pig myelin basic protein immunization)[1]
Dosage: 0.01 mg/kg; 0.1 mg/kg
Administration: p.o.; single dose
Result: Did not significantly impact clinical disease scores at 0.01 mg/kg vs vehicle.
Delayed disease onset and produced a statistically significant reduction in clinical disease scores at 0.1 mg/kg vs vehicle.
Molecular Weight

459.54

Formula

C26H22FN3O2S
CAS No.
SMILES

O=C(O)C1CN(CC2=CC=C(C(F)=C2)C3=NC=4C=CC(=NC4S3)C5(C=6C=CC=CC6)CC5)C1
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.

AMG 369 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:

AMG 3691202073-26-4AMG369AMG-369LPL ReceptorLysophospholipid ReceptorS1P2multiple sclerosisS1P5S1P4U2OS cellsratS1P1lymphocytesexperimental autoimmune encephalomyelitisS1P3Inhibitorinhibitorinhibit

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:
AMG 369
Cat. No.:
HY-14402
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.