BCX 1470 methanesulfonateSerine protease inhibitor CAS# 217099-44-0 |
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Quality Control & MSDS
3D structure
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| Cas No. | 217099-44-0 | SDF | Download SDF |
| PubChem ID | 9822204 | Appearance | Powder |
| Formula | C15H14N2O5S3 | M.Wt | 398.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | BCX 1470 | ||
| Solubility | DMSO : ≥ 33.33 mg/mL (83.64 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (2-carbamimidoyl-1-benzothiophen-6-yl) thiophene-2-carboxylate;methanesulfonic acid | ||
| SMILES | CS(=O)(=O)O.C1=CSC(=C1)C(=O)OC2=CC3=C(C=C2)C=C(S3)C(=N)N | ||
| Standard InChIKey | MCPAUXMAIOICMC-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]
Target: Factor D; C1s
BCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat. References: | |||||
BCX 1470 methanesulfonate Dilution Calculator
BCX 1470 methanesulfonate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5095 mL | 12.5477 mL | 25.0954 mL | 50.1907 mL | 62.7384 mL |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0191 mL | 10.0381 mL | 12.5477 mL |
| 10 mM | 0.251 mL | 1.2548 mL | 2.5095 mL | 5.0191 mL | 6.2738 mL |
| 50 mM | 0.0502 mL | 0.251 mL | 0.5019 mL | 1.0038 mL | 1.2548 mL |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.251 mL | 0.5019 mL | 0.6274 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BCX 1470 is a serine protease inhibitor with the IC50 of 96 nM for factor D and 1.6 nM for C1s [1].
Serine proteases are enzymes that cleave peptide bonds in proteins which are found ubiquitously in both eukaryotes and prokaryotes and serine serves as the nucleophilic amino acid at the active site. According to structure, serine proteases are divided into trypsin-like (chymotrypsin-like) family and subtilisin-like family. It is reported that serine proteases play an important role in various physiological functions, including digestion, immune response, blood coagulation and reproduction. [2] [3].
BCX 1470 is a potent serine protease inhibitor and functions on the complement enzymes CIs and factor D sites. By determining the ability of enzyme to hydrolyze appropriate synthetic substrates, the result showed that BCX 1470 inhibited the factor D and C1s esterolytic activity which were important in the function of serine protease [1].
In induced dermal RPA reaction rat model, administration of BCX 1470 markedly abbrogated the RPA reaction via inhibiting edema development and complement activity by inactivation of C1s and factor D enzymatic activity [1].
It is also reported that BCX 1470 inhibited Trypsin with the IC50 value of 326 nM [1].
References:
[1]. Szalai, A.J., et al., The Arthus reaction in rodents: species-specific requirement of complement. J Immunol, 2000. 164(1): p. 463-8.
[2]. Srivastava, A. and Q. Dong, Regulation of a serine protease homolog by the JNK pathway during thoracic development of Drosophila melanogaster. FEBS Open Bio, 2015. 5: p. 117-23.
[3]. Yamasaki, K., et al., Increased serine protease activity and cathelicidin promotes skin inflammation in rosacea. Nat Med, 2007. 13(8): p. 975-80.
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