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Art. -Nr.: HY-P11882

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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. Nr.: 947545-69-9
Formel: C₁₄₄H₂₀₀N₃₈O₃₂S₄
Molecular Weight:3103.62

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

SYN1436 Chemical Structure

CAS. Nr.: 947545-69-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 K_d 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.

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.

Chemical Information

CAS. Nr. 947545-69-9
Molecular Weight 3103.62
Formel C₁₄₄H₂₀₀N₃₈O₃₂S₄
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
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)
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mezo AR, et al. Reduction of IgG in nonhuman primates by a peptide antagonist of the neonatal Fc receptor FcRn. Proc Natl Acad Sci U S A. 2008 Feb 19;105(7):2337-42. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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