| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Edratide targets immune pathways involved in systemic lupus erythematosus (SLE). It downregulates pathogenic cytokines, apoptosis, and IFN-alpha gene expression. It upregulates immunosuppressive molecules and Tregs in peripheral blood. Edratide reduces the rates of apoptosis and downregulates caspase-8 and caspase-3, while upregulating Bcl-xL. Its mechanism of action involves modulation of the immune response to restore immune tolerance.
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| ln Vitro |
In vitro studies demonstrate that Edratide reduces the rates of apoptosis and downregulates caspase-8 and caspase-3, while upregulating Bcl-xL. It downregulates pathogenic cytokines, apoptosis, and IFN-alpha gene expression. Its in vitro activity is assessed in immune cells (e.g., peripheral blood mononuclear cells) from SLE patients or healthy donors. Cytokine production is measured by ELISA or multiplex assays. Apoptosis is assessed by flow cytometry or caspase activity assays. Gene expression is measured by qPCR.
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| ln Vivo |
Edratide (20-50 µg; subcutaneous injection; once weekly for 10 weeks) exhibits therapeutic effects on SLE by modulating gene expression [2]. Edratide (50 μg/mouse; subcutaneous injection; 10 times a week) can lower the apoptotic rate of SLE mice, downregulate caspase-8 and caspase-3, and upregulate Bcl-xL [3].
In vivo studies have confirmed the data from animal models, showing that Edratide downregulates pathogenic cytokines, apoptosis, and IFN-alpha gene expression, and upregulates immunosuppressive molecules and Tregs in peripheral blood. In a study, Edratide (20-50 microg; s.c.; once a week for 10 weeks) exerted beneficial effects on SLE through regulation of gene expression. The compound has shown potential for the treatment of SLE. |
| Enzyme Assay |
In vitro assays for Edratide involve measuring its effects on immune cells. Peripheral blood mononuclear cells (PBMCs) from SLE patients or healthy donors are treated with the compound. Cytokine production (e.g., IFN-alpha, IL-6, TNF-alpha) is measured by ELISA or multiplex assays. Apoptosis is assessed by flow cytometry using Annexin V/PI staining or by measuring caspase-8 and caspase-3 activity. Bcl-xL expression is measured by Western blotting or qPCR. Treg cell populations are analyzed by flow cytometry using FoxP3 staining.
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| Cell Assay |
Cellular assays for Edratide are conducted using immune cells such as PBMCs or purified T cells. Cells are treated with varying concentrations of the compound for 24-72 hours. Cytokine production is measured in culture supernatants by ELISA. Apoptosis is assessed by flow cytometry using Annexin V/PI staining. Caspase-8 and caspase-3 activity is measured using fluorogenic substrates. Bcl-xL expression is assessed by Western blotting or qPCR. Treg cell populations are analyzed by flow cytometry.
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| Animal Protocol |
Animal/Disease Models: 6-7 month female mice (confirmed SLE) [2]
Doses: 20-50 µg Route of Administration: subcutaneous injection; once a week for 10 weeks Experimental Results: Up-regulation of Tnfsf4, Il5ra, Zbtb20, Nid1 RNA transcripts that downregulate Tfpi and S100a8 transcripts. Animal/Disease Models: 7-8 months old BWF1 female mice with SLE [3] Doses: 50 μg/mouse Route of Administration: Sc; 10-week Experimental Results: diminished apoptosis, downregulation of caspase-8 and caspase-3, Bcl-xL is upregulated. In vivo animal studies with Edratide have been conducted in animal models of SLE. In a study, Edratide (20-50 microg; s.c.; once a week for 10 weeks) exerted beneficial effects on SLE through regulation of gene expression. Animal models of SLE (e.g., MRL/lpr mice, NZB/W F1 mice) are used. Animals are treated with the compound via subcutaneous injection. Disease progression is monitored by measuring proteinuria, anti-dsDNA antibody levels, and survival. Cytokine and gene expression are assessed in tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Edratide Acetate have not been extensively characterized. The compound has a molecular weight of 2309.53 and a molecular formula of C111H14₉N2₇O2₈. The acetate salt form enhances solubility. As a 19-amino acid peptide, Edratide has poor oral bioavailability and is typically administered by subcutaneous injection. The compound is typically stored at -20degC.
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| Toxicity/Toxicokinetics |
Toxicological data for Edratide Acetate are limited. The compound is not intended for human therapeutic use and is supplied for research purposes only. In animal studies, the compound has been administered at doses of 20-50 microg via subcutaneous injection. The compound is generally well-tolerated at these doses. Standard safety precautions should be followed when handling this compound.
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| References |
[1]. Urowitz MB, et al. Safety and efficacy of hCDR1 (Edratide) in patients with active systemic lupus erythematosus: results of phase II study. Lupus Sci Med. 2015 Aug 11;2(1):e000104.
[2]. Elmann A, et al. Altered gene expression in mice with lupus treated with edratide, a peptide that ameliorates the disease manifestations. Arthritis Rheum. 2007 Jul;56(7):2371-81. [3]. Sharabi A, et al. The role of apoptosis in the ameliorating effects of a CDR1-based peptide on lupus manifestations in a mouse model. J Immunol. 2007 Oct 15;179(8):4979-87. |
| Additional Infomation |
Edratide is being studied in the clinical trial NCT00203151 (a study evaluating the tolerability, safety and efficacy of edratide in the treatment of lupus).
Edratide Acetate is a synthetic tolerogenic peptide based on the CDR1 of a human anti-DNA antibody, with potential for the treatment of SLE. It downregulates pathogenic cytokines, apoptosis, and IFN-alpha, and upregulates immunosuppressive molecules and Tregs. It reduces apoptosis and downregulates caspase-8 and caspase-3, while upregulating Bcl-xL. The compound is not an FDA-approved drug and has no clinical indications. It is available in high purity and is typically stored at -20degC. |
| Molecular Formula |
C111H149N27O28
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|---|---|
| Molecular Weight |
2309.53000
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| Exact Mass |
2308.11
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| CAS # |
433922-67-9
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| PubChem CID |
16214485
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| Appearance |
White to off-white solid powder
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| LogP |
5.625
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| Hydrogen Bond Donor Count |
31
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| Hydrogen Bond Acceptor Count |
31
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| Rotatable Bond Count |
68
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| Heavy Atom Count |
166
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| Complexity |
5190
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| Defined Atom Stereocenter Count |
17
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| SMILES |
NCCCC[C@H](NC(CNC([C@H]1N(C([C@H]2N(C(CNC(CNC=O)=O)=O)CCC2)=O)CCC1)=O)=O)C(NCC(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC1C2=CC=CC=C2NC=1)C(N[C@@H]([C@@H](C)CC)C(NCC(O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
VXXZQHUWZSRPAM-CDJUQFLLSA-N
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| InChi Code |
InChI=1S/C111H149N27O28/c1-5-59(3)94(107(163)123-57-93(150)151)135-103(159)82(49-64-53-119-72-22-11-8-19-69(64)72)131-99(155)77(38-41-92(148)149)127-98(154)76(37-40-91(146)147)125-89(144)55-121-96(152)74(24-13-14-42-112)124-90(145)56-122-106(162)85-26-16-44-137(85)110(166)86-27-17-45-138(86)109(165)78(36-39-87(114)142)129-97(153)75(25-15-43-117-111(115)116)128-108(164)95(60(4)6-2)136-104(160)83(50-65-54-120-73-23-12-9-20-70(65)73)133-105(161)84(58-139)134-102(158)81(48-63-52-118-71-21-10-7-18-68(63)71)132-101(157)80(47-62-30-34-67(141)35-31-62)130-100(156)79(126-88(143)51-113)46-61-28-32-66(140)33-29-61/h7-12,18-23,28-35,52-54,59-60,74-86,94-95,118-120,139-141H,5-6,13-17,24-27,36-51,55-58,112-113H2,1-4H3,(H2,114,142)(H,121,152)(H,122,162)(H,123,163)(H,124,145)(H,125,144)(H,126,143)(H,127,154)(H,128,164)(H,129,153)(H,130,156)(H,131,155)(H,132,157)(H,133,161)(H,134,158)(H,135,159)(H,136,160)(H,146,147)(H,148,149)(H,150,151)(H4,115,116,117)/t59-,60-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,94-,95-/m0/s1
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| Chemical Name |
(4S)-4-[[2-[[(2S)-6-amino-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]hexanoyl]amino]acetyl]amino]-5-[[(2S)-4-carboxy-1-[[(2S)-1-[[(2S,3S)-1-(carboxymethylamino)-3-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxobutan-2-yl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~43.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4330 mL | 2.1649 mL | 4.3299 mL | |
| 5 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | |
| 10 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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