BMS-962212
Based on 1 Customer Validation
BMS-962212 is a factor XIa (FXIa) inhibitor with a Ki of 0.7 nM against human FXIa and a Ki of 3 nM against rabbit FXIa. BMS-962212 blocks thrombosis while preserving normal hemostatic function. BMS-962212 is applicable to thrombosis-related research.
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- Pureté: 99.33%
- CAS No.: 1430114-34-3
- Formule: C32H28ClFN8O5
- Masse moléculaire:659.07
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
BMS-962212 (Compound 55) at a concentration of 0.3 μM prolongs the activated partial thromboplastin time in human plasma by 1.5-fold, indicating that it possesses in vitro anticoagulant activity[1].
BMS-962212 exhibits high selectivity for FXIa and inhibits rabbit activated plasma kallikrein with a Ki of 1100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | AUCall | T1/2 |
|---|---|---|---|---|---|---|
| Rat[1] | 0.5 mg/kg | i.v. | 31 mL/min/kg | 0.32 L/kg | 441 nM·h | 0.22 h |
| Rabbit[1] | 0.5 mg/kg | i.v. | 43 mL/min/kg | 0.71 L/kg | 270 nM·h | 0.6 h |
| Dog[1] | 4.75 mg/kg | i.v. | 15 mL/min/kg | 1.02 L/kg | 7757 nM·h | 1.05 h |
| Cynomolgus Monkey[1] | 2.03 mg/kg | i.v. | 31 mL/min/kg | 1.16 L/kg | 1590 nM·h | 0.78 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rabbit[1]
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Dosage:0.23 mg/kg (bolus) + 1.55 mg/kg/h (infusion); 0.46 mg/kg (bolus) + 3.1 mg/kg/h (infusion)
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Administration:i.v. bolus; i.v. infusion
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Result:Inhibited thrombus formation by 83%.
Increased activated partial thromboplastin time (aPTT) up to 1.8-fold over baseline.
Caused no changes in prothrombin time (PT).
Did not increase bleeding time compared to vehicle at twice the antithrombotic dose.
Resulted in bleeding times not greater than with aspirin treatment alone when combined with aspirin (4 mg/kg/h i.v.).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1430114-34-3
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Appearance Solid
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Masse moléculaire 659.07
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Formule C32H28ClFN8O5
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Color Off-white to light yellow
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SMILES
ClC1=C(F)C(/C=C/C(N2[C@H](C(NC3=CC=C(C(O)=O)C=C3)=O)C(C=CC=C4N5C(CN(C)CC5)=O)=C4CC2)=O)=C(N6C=NN=N6)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 250 mg/mL (379.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5173 mL | 7.5864 mL | 15.1729 mL | 37.9322 mL |
| 5 mM | 0.3035 mL | 1.5173 mL | 3.0346 mL | 7.5864 mL | |
| 10 mM | 0.1517 mL | 0.7586 mL | 1.5173 mL | 3.7932 mL | |
| 15 mM | 0.1012 mL | 0.5058 mL | 1.0115 mL | 2.5288 mL | |
| 20 mM | 0.0759 mL | 0.3793 mL | 0.7586 mL | 1.8966 mL | |
| 25 mM | 0.0607 mL | 0.3035 mL | 0.6069 mL | 1.5173 mL | |
| 30 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2644 mL | |
| 40 mM | 0.0379 mL | 0.1897 mL | 0.3793 mL | 0.9483 mL | |
| 50 mM | 0.0303 mL | 0.1517 mL | 0.3035 mL | 0.7586 mL | |
| 60 mM | 0.0253 mL | 0.1264 mL | 0.2529 mL | 0.6322 mL | |
| 80 mM | 0.0190 mL | 0.0948 mL | 0.1897 mL | 0.4742 mL | |
| 100 mM | 0.0152 mL | 0.0759 mL | 0.1517 mL | 0.3793 mL |
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