BM 567 |
| رقم الكتالوجGC14758 |
dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and as an antagonist of the TP receptor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 284464-77-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IC50: 1.1 nM for TXA2 receptor antagonism
BM 567 is acting as an inhibitor of thromboxane A2 (TXA2) synthase and an antagonist of the TP receptor.
Thromboxane A2 (TXA2), a potent thrombogenic and vasoconstrictor eicosanoid, is produced in large quantities by activated platelets. TXA2 has been reported as a causal factor in the onset of stroke and myocardial infarction.
In vitro: BM 567 was identified as a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and an antagonist of the TP receptor, the G protein-coupled receptor mediating TXA2 activity in platelets and vascular smooth muscle. BM 567 antagonized the vascular smooth muscle TP receptor with an IC50 value of 1.1 nM. BM 567 was also able to inhibit platelet TX synthase with an IC50 value of 12 nM. In addition, by comparing crystallographic and electronic properties of BM567 and terbogrel, two compounds with dual action (TXRA and TXSI), two essential anchoring identified: sulfonyl and nitro group for BM567 and carboxylate and pyridine nitrogen for terbogrel [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Michaux, C. ,Rolin, S.,Dogné, J.M., et al. Structure determination and comparison of BM567, a sulfonylurea, with Terbogrel, two compounds with dual action, thromboxane receptor antagonism, and thromboxane synthase inhibition. Bioorganic & Medicinal Chemistry Letters 11, 1019-1022 (2001).
| Cas No. | 284464-77-3 | SDF | |
| Chemical Name | 2-(cyclohexylamino)-5-nitro-N-[(pentylamino)carbonyl]-benzenesulfonamide | ||
| Canonical SMILES | CCCCCNC(=O)NS(=O)(=O)c1cc(ccc1NC1CCCCC1)[N](=O)O | ||
| Formula | C18H28N4O5S | M.Wt | 412.5 |
| الذوبان | ≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4242 mL | 12.1212 mL | 24.2424 mL |
| 5 mM | 484.8 μL | 2.4242 mL | 4.8485 mL |
| 10 mM | 242.4 μL | 1.2121 mL | 2.4242 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *