SYN1436
SYN1436 is a selective human neonatal Fc receptor (hFcRn) antagonist with an IC50 of 2.4 nM. SYN1436 binds to hFcRn and inhibits hFcRn-hIgG interaction. SYN1436 can be used for the research of autoimmune diseases.
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- CAS No.: 947545-69-9
- Formule: C144H200N38O32S4
- Masse moléculaire:3103.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
SYN1436 (2.4 nM; 2 h) potently inhibits the hIgG-shFcRn interaction in an ELISA format at pH 6, with an IC50 of 2.4 nM[1].
SYN1436 (2.8 nM; 1 h) potently inhibits hIgG binding to hFcRn-expressing 293c11 cells in a FACS-based competition assay at pH 6, with an IC50 of 2.8 nM[1].
SYN1436 (0.04-20 nM) binds with extremely high affinity to immobilized shFcRn at both pH 6 and pH 7.4, with Kd values of <0.5 nM and <0.8 nM, respectively[1].
SYN1436 does not inhibit the shFcRn-HSA interaction at pH 6 at a concentration of 10 μM, nor does it bind directly to HSA at concentrations up to 100 μM at pH 6 or pH 7.4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SYN1436 (1-5 mg/kg; s.c. or i.v.; once weekly or three times weekly; up to 4 weeks) dose-dependently reduces endogenous serum IgG levels in cynomolgus monkeys without altering albumin, IgM, or IgA levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TG32B (muFcRn -/- , muβ2m -/- , huFcRn +/+ , huβ2m +/+ transgenic strain)[1]
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Dosage:0.5 mg/kg; 1 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; once daily; 4 days
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Result:Reduced serum hIgG levels in a dose-dependent manner at 120 h.
Reduced hIgG levels by 90% compared to vehicle control at 10 mg/kg dose.
Shortened the serum half-life of hIgG from 114 h (vehicle control) to 34 h at 10 mg/kg dose.
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Animal Model:Cynomolgus monkeys (average body weight 4.2 kg)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:s.c. (once weekly for 4 doses or three times weekly for 12 doses); i.v. (three times weekly for 12 doses or three times weekly for 7 doses); up to 4 weeks
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Result:Reduced serum IgG by ~30% over 4 weeks with weekly s.c. dosing of 1 mg/kg.
Reduced serum IgG by 60% over 4 weeks with three-times-weekly s.c. or i.v. dosing of 1 mg/kg.
Reduced serum IgG by ~50% over 4 weeks with weekly s.c. dosing of 5 mg/kg.
Reduced serum IgG by 60% over 4 weeks with three-times-weekly s.c. dosing of 5 mg/kg.
Reduced serum IgG by up to 80% after 2.5 weeks of treatment with three-times-weekly i.v. dosing of 5 mg/kg.
Restored serum IgG levels to pretreatment or near-pretreatment levels after treatment cessation.
Had no effect on serum albumin, IgM, or IgA concentrations, with levels remaining within ~20% of predose values.
Chemical Information
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CAS No. 947545-69-9
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Masse moléculaire 3103.62
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Formule C144H200N38O32S4
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SMILES
O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](C(C)(SSC[C@@H](C(N)=O)NC2=O)C)C(N[C@@H]([C@H](O)C)C(NCC(N[C@@H](CC3=CNC=N3)C(N[C@@H](CC4=CC=CC=C4)C(NCC(N(C)CC(N(C)[C@@H](CC(C)C)C(N[C@@H](CC5=CC=C(C=C5)O)C(N6[C@H]2CCC6)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC(N[C@H](C(N[C@H](C(N[C@H]7C(C)(C)SSC[C@H](NC([C@@H]8CCCN8C([C@@H](NC([C@@H](N(C(CN(C)C(CNC([C@@H](NC([C@@H](NC(CNC([C@@H](NC7=O)[C@@H](C)O)=O)=O)CC9=CNC=N9)=O)CC%10=CC=CC=C%10)=O)=O)=O)C)CC(C)C)=O)CC%11=CC=C(O)C=C%11)=O)=O)C(N)=O)=O)CC%12=CC=CC=C%12)=O)CCCNC(N)=N)=O
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Sequence
Arg-Phe-Pen-Thr-Gly-His-Phe-Gly-Sar-{NMeLeu}-Tyr-Pro-Cys-NH2 (disulfide bridge:Pen3-Cys13) (Arg1-Arg1' succinic acid dimer)
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Sequence Shortening
RF-Pen-TGHFG-Sar-{NMeLeu}-YPC-NH2 (disulfide bridge:Pen3-Cys13) (Arg1-Arg1' succinic acid dimer)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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