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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- CAS No.: 1354060-46-0
- 화학식: C20H27ClN2O3
- 분자량:378.89
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
|
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 |
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 (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.
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Animal Model:LEW/SsNHsd (male, 180-200 g, LPS-induced)[1]
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Dosage:1%
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Administration:topical
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Result:Reduced aqueous humor protein concentration to <20 mg/mL vs vehicle control.
Significantly reduced leukocyte infiltration into the anterior chamber.
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Animal Model:Dutch Belted pigmented (male/female, 2.5-3 kg, Arachidonic acid-induced)[1]
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Dosage:0.1%; 0.3%
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Administration:topical
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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.
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Animal Model:Chlorocebus sabaeus (8 males, 7 females, 3.2-6.7 kg, phacoemulsification surgery-induced)[1]
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Dosage:0.3%
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Administration:topical; twice daily
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Result:Reduced laser flare responses by ~50% relative to PBS-treated controls on day 1 post-surgery.
Chemical Information
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CAS No. 1354060-46-0
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분자량 378.89
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화학식 C20H27ClN2O3
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SMILES
O=C(CCC1=NN(CC2=CC(Cl)=CC=C2OCC(CC)CC)C(C)=C1)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGN 225660 Related Classifications
HY-183037 Related Classifications
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