BCX 1470Serine protease inhibitor CAS# 217099-43-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 217099-43-9 | SDF | Download SDF |
| PubChem ID | 9822205 | Appearance | Powder |
| Formula | C14H10N2O2S2 | M.Wt | 302.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Thrombin inhibitor | ||
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Chemical Name | (2-carbamimidoyl-1-benzothiophen-6-yl) thiophene-2-carboxylate | ||
| SMILES | C1=CSC(=C1)C(=O)OC2=CC3=C(C=C2)C=C(S3)C(=N)N | ||
| Standard InChIKey | OTGQTQBPQCRNRG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H10N2O2S2/c15-13(16)12-6-8-3-4-9(7-11(8)20-12)18-14(17)10-2-1-5-19-10/h1-7H,(H3,15,16) | ||
| 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 Dilution Calculator
BCX 1470 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.3071 mL | 16.5355 mL | 33.071 mL | 66.1419 mL | 82.6774 mL |
| 5 mM | 0.6614 mL | 3.3071 mL | 6.6142 mL | 13.2284 mL | 16.5355 mL |
| 10 mM | 0.3307 mL | 1.6535 mL | 3.3071 mL | 6.6142 mL | 8.2677 mL |
| 50 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.3228 mL | 1.6535 mL |
| 100 mM | 0.0331 mL | 0.1654 mL | 0.3307 mL | 0.6614 mL | 0.8268 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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IC50: FD 96 nM, C1 1.6 nM
C1s is an 80-kDa serine protease that mediates the proteolytic activity of the C1 complex by cleaving C2 and C4 both. BCX-1470, discovered in 1997 as a FD inhibitor (IC50=96 nM), was further found to be a very potent C1s inhibitor (IC50=1.6 nM).
In vitro: BCX-1470 has the highest inhibitory activity of Factor D, with an IC50 of approx. 100 nM, which is two orders higher than the inhibitory activity of another commercially available general protease inhibitor, named FUT-175, when inhibting FD [1].
In vivo: BCX-1470 has been shown to be safe in animal toxicity studies and has blocked the development of reverse-passive Arthus reactioninduced oedema in rats [1].
Clinical trial: BCX-1470 has also been tested for safety in clinical trials with healthy volunteers but the outcome of these trials have not officially been published. Whereas no further clinical trials have been reported, a recent patent might indicate a future usage of the compound in the treatment of AMD. It suggests that BCX-1470 would be a candidate therapeutic for complement activation during cardiopulmonary bypass surgery
Reference:
[1] Morikis D, Lambris JD. Structural aspects and design of low-molecular-mass complement inhibitors. Biochem Soc Trans. 2002;30(Pt 6):1026-36.
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The Arthus reaction in rodents: species-specific requirement of complement.[Pubmed:10605043]
J Immunol. 2000 Jan 1;164(1):463-8.
We induced reverse passive Arthus (RPA) reactions in the skin of rodents and found that the contribution of complement to immune complex-mediated inflammation is species specific. Complement was found to be necessary in rats and guinea pigs but not in C57BL/6J mice. In rats, within 4 h after initiation of an RPA reaction, serum alternative pathway hemolytic titers decreased significantly below basal levels, whereas classical pathway titers were unchanged. Thus the dermal reaction proceeds coincident with systemic activation of complement. The serine protease inhibitor BCX 1470, which 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. These data support the proposal that complement-mediated processes are of major importance in the Arthus reaction in rats and guinea pigs, and suggest that BCX 1470 will be useful as an anti-inflammatory agent in diseases where complement activation is known to be detrimental.
