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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
The primary targets of BCX 1470 methanesulfonate are complement factor D and C1s. Factor D is a serine protease essential for the alternative complement pathway, while C1s is a serine protease involved in the classical complement pathway. By inhibiting these enzymes, the compound blocks complement activation and may be useful for treating complement-mediated diseases.
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| ln Vitro |
BCX 1470 mesylate is a serine protease inhibitor. BCX 1470 mesylate inhibits the esterolytic and hemolytic activities of complement enzymes Cls and factor D in vitro and prevents RPA-induced edema in rats.
In vitro, BCX 1470 methanesulfonate inhibits the esterolytic and hemolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM). It is a potent inhibitor of these complement enzymes. It has also been described as a potent and selective inhibitor of dipeptidyl peptidase II (DPP II). Its activity makes it a valuable tool for studying the complement system. |
| ln Vivo |
In vivo, BCX 1470 methanesulfonate has been shown to block the development of RPA-induced edema in the rat. This demonstrates its in vivo efficacy in a model of inflammation. Its ability to inhibit complement activation suggests potential for treating inflammatory and autoimmune diseases.
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| Enzyme Assay |
For complement enzyme assays, the esterolytic or hemolytic activity of purified factor D or C1s is measured. The enzyme is incubated with varying concentrations of BCX 1470 methanesulfonate and a chromogenic or fluorogenic substrate. The reaction is monitored, and IC50 values are calculated. For hemolytic assays, the ability of the compound to inhibit complement-mediated lysis of red blood cells is measured.
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| Cell Assay |
For cellular studies, immune cells are cultured and stimulated to activate the complement pathway. BCX 1470 methanesulfonate is added, and the production of complement components or inflammatory mediators is measured. For mechanistic studies, signaling pathways are analyzed by Western blot.
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| Animal Protocol |
For in vivo efficacy studies, animal models of complement-mediated inflammation are used. BCX 1470 methanesulfonate is formulated in vehicle and administered intraperitoneally or intravenously. Inflammation is assessed by measuring edema, inflammatory cell infiltration, and cytokine levels.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BCX 1470 methanesulfonate are not extensively reported. As a small molecule, it is expected to have moderate oral bioavailability. Its metabolism likely involves hepatic CYP450 enzymes. A comprehensive PK study would be needed for any potential therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for BCX 1470 methanesulfonate are limited. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research compounds, appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
BCX 1470 methanesulfonate (CAS 217099-44-0) is a serine protease inhibitor that targets complement factor D (IC50=96 nM) and C1s (IC50=1.6 nM). It has the molecular formula C₁₅H₁₄N₂O₅S₃ and a molecular weight of 398.48. It blocks RPA-induced edema in rats and is strictly for research use.
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| Molecular Formula |
C14H10N2O2S2.CH4O3S
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|---|---|
| Molecular Weight |
398.47706
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| Exact Mass |
398.006
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| CAS # |
217099-44-0
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| Related CAS # |
BCX 1470;217099-43-9
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| PubChem CID |
9822204
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| Appearance |
White to off-white solid powder
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| Boiling Point |
509.9ºC at 760 mmHg
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| Flash Point |
262.2ºC
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| LogP |
4.85
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)O.C1=CSC(=C1)C(=O)OC2=CC3=C(C=C2)C=C(S3)C(=N)N
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| InChi Key |
MCPAUXMAIOICMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N2O2S2.CH4O3S/c15-13(16)12-6-8-3-4-9(7-11(8)20-12)18-14(17)10-2-1-5-19-10;1-5(2,3)4/h1-7H,(H3,15,16);1H3,(H,2,3,4)
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| Chemical Name |
(2-carbamimidoyl-1-benzothiophen-6-yl) thiophene-2-carboxylate;methanesulfonic 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, avoid exposure to moisture. |
| 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 : ≥ 33.33 mg/mL (~83.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 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 (6.27 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 (6.27 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 | 2.5095 mL | 12.5477 mL | 25.0954 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0191 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5095 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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