2. Immunology/Inflammation
  3. Fc Receptor (FcR)
  4. 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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SYN1436

SYN1436 Chemical Structure

CAS No. : 947545-69-9

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SYN1436 Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

SYN1436 (0.5-10 mg/kg; i.v.; once daily; 4 days) increases hIgG catabolism in human FcRn transgenic mice in a dose-dependent manner, with the 10 mg/kg dose reducing hIgG levels by 90% and shortening hIgG half-life to 34 h[1].
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.

Animal Model: TG32B (muFcRn -/- , muβ2m -/- , huFcRn +/+ , huβ2m +/+ transgenic strain)[1]
Dosage: 0.5 mg/kg; 1 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; once daily; 4 days
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.
Animal Model: Cynomolgus monkeys (average body weight 4.2 kg)[1]
Dosage: 1 mg/kg; 5 mg/kg
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
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.
Molecular Weight

3103.62

Formula

C144H200N38O32S4
CAS No.
Sequence

Arg-Phe-Pen-Thr-Gly-His-Phe-Gly-Sar-{NMeLeu}-Tyr-Pro-Cys-NH2 (disulfide bridge:Pen3-Cys13) (Arg1-Arg1' succinic acid dimer)
Sequence Shortening

RF-Pen-TGHFG-Sar-{NMeLeu}-YPC-NH2 (disulfide bridge:Pen3-Cys13) (Arg1-Arg1' succinic acid dimer)
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
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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SYN1436 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:

SYN1436947545-69-9SYN 1436SYN-1436Fc Receptor (FcR)Fc ReceptorIgG catabolismIgMalbumincynomolgus monkeyshuman neonatal Fc receptorhFcRn transgenic micehFcRnautoimmune diseaseshIgG293c11 cellsInhibitorinhibitorinhibit

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