SYN1436
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.64%
- CAS No.: 947545-69-9
- Formule: C144H200N38O32S4
- Masse moléculaire:3103.62
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Stockage:
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)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- 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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Appearance Solid
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Masse moléculaire 3103.62
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Formule C144H200N38O32S4
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Color White to off-white
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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
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)
Solvant et solubilité
DMSO : 100 mg/mL (32.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (0.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (0.81 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (287 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.3222 mL | 1.6110 mL | 3.2220 mL | 8.0551 mL |
| 5 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6110 mL | |
| 10 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL | |
| 15 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL | |
| 20 mM | 0.0161 mL | 0.0806 mL | 0.1611 mL | 0.4028 mL | |
| 25 mM | 0.0129 mL | 0.0644 mL | 0.1289 mL | 0.3222 mL | |
| 30 mM | 0.0107 mL | 0.0537 mL | 0.1074 mL | 0.2685 mL |
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