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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.

CAS No.: 1202073-26-4
Formula: C₂₆H₂₂FN₃O₂S
Molecular Weight:459.54

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AMG 369 Chemical Structure

CAS No.: 1202073-26-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

S1PR1

S1PR5

S1PR3

All LPL Receptor Isoforms :

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.

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.

Chemical Information

CAS No. 1202073-26-4
Molecular Weight 459.54
Formula C₂₆H₂₂FN₃O₂S
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

Handling Instructions (2659 KB)

References

[1]. Cee V J, et al. Discovery of AMG 369, a Thiazolo [5, 4-b] pyridine Agonist of S1P1 and S1P5[J]. ACS Medicinal Chemistry Letters, 2011, 2(2): 107-112.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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