Icotrokinra acetate
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.
For research use only. We do not sell to patients.
- Formula: C90H120N20O22S2·xC2H4O2
- Molecular Weight:1898.17 (free base)
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
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IL-23 7.1 pM (Kd) |
Icotrokinra (1-30 mg/kg; p.o.; twice daily for 3 days) acetate prevents IL-23-induced upregulation of IL-17A and IL-22 in a rat skin inflammation model at doses greater than 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Molecular Weight 1898.17 (free base)
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Formula C90H120N20O22S2·xC2H4O2
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Color White to off-white
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Synonyms
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
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Sequence
Ac-Pen-Asn-Thr-Trp(7-Me)-Lys(Ac)-Pen-Phe(4-amino ethoxy)-2Nal-ThpGly-Glu-Asn-3Pal-Sar-NH2 (Pen1&Pen6 bridge)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)