2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. AGN 225660

AGN 225660 is a multi-prostanoid receptor antagonist with human IC50 values of 70, 70, 5, 220 and 180 nM for EP1, EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis.

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AGN 225660

AGN 225660 Chemical Structure

CAS No. : 1354060-46-0

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AGN 225660 Related Antibodies

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DP EP FP IP TXA2/TP TXB2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

AGN 225660 is a multi-prostanoid receptor antagonist with human IC50 values of 70, 70, 5, 220 and 180 nM for EP1, EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis[1].

IC50 & Target[1]

TP

5 nM (IC50)

EP1

70 nM (IC50)

EP4

70 nM (IC50)

FP

180 nM (IC50)

DP1

220 nM (IC50)

IL-8

 

IL-12

 

IL-23

 

In Vitro

AGN 225660 potently antagonizes pro-inflammatory human recombinant prostanoid receptors (EP1, EP4, TP, DP1, FP) with IC50 values ranging from 5 to 220 nM, and has weak activity at anti-inflammatory receptors (EP2, EP3, IP) with IC50 values ≥1100 nM in HEK-293 transfectants[1].
AGN 225660 (1-10 μM; 24 h) dose-dependently and significantly inhibits TNFα-induced IL-8, MCP-1, and RANTES secretion in human monocyte-derived
dendritic cells[1].
AGN 225660 (1-10 μM; 18-20 h) significantly inhibits LPS (HY-D1056)-induced IL-12p70 and IL-23 secretion by 65-75% in human monocyte-derived
dendritic cells[1].

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

AGN 225660 Related Antibodies
In Vivo

AGN 225660 (1%; topical) significantly reduces protein exudation and leukocyte infiltration in LPS (HY-D1056)-induced eyes uveitis in Lewis rats[1].
AGN 225660 (0.1-0.3%; topical) completely inhibits leukocyte infiltration in Arachidonic acid (HY-109590)-induced uveitis in Dutch Belted rabbits at the 0.3% dose[1].
AGN 225660 (0.3%; topical; twice daily) reduces phacoemulsification surgery-induced anterior chamber flare by ~50% in African green monkeys[1].

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

Animal Model: LEW/SsNHsd (male, 180-200 g, LPS-induced)[1]
Dosage: 1%
Administration: topical
Result: Reduced aqueous humor protein concentration to <20 mg/mL vs vehicle control.
Significantly reduced leukocyte infiltration into the anterior chamber.
Animal Model: Dutch Belted pigmented (male/female, 2.5-3 kg, Arachidonic acid-induced)[1]
Dosage: 0.1%; 0.3%
Administration: topical
Result: Produced marginal inhibition of leukocyte infiltration at 0.1% dose.
Totally inhibited arachidonic acid-induced leukocyte infiltration into the anterior chamber at 0.3% dose.
Animal Model: Chlorocebus sabaeus (8 males, 7 females, 3.2-6.7 kg, phacoemulsification surgery-induced)[1]
Dosage: 0.3%
Administration: topical; twice daily
Result: Reduced laser flare responses by ~50% relative to PBS-treated controls on day 1 post-surgery.
Molecular Weight

378.89

Formula

C20H27ClN2O3
CAS No.
SMILES

O=C(CCC1=NN(CC2=CC(Cl)=CC=C2OCC(CC)CC)C(C)=C1)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
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AGN 225660 Related Classifications

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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:

AGN 2256601354060-46-0AGN225660AGN-225660Prostaglandin ReceptorInterleukin RelatedILuveitisDP1TPIL-8MCP-1EP4EP1FPRANTESIL-12p70Inhibitorinhibitorinhibit

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