2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. BMS-962212

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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BMS-962212

BMS-962212 構造式

CAS 番号 : 1430114-34-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 2102 在庫あり
Solution
10 mM * 1 mL in DMSO USD 2102 在庫あり
Solid
1 mg $580 在庫あり
5 mg $1450 在庫あり
10 mg $2350 在庫あり
25 mg $4340 在庫あり
50 mg $6500 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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Other Forms of BMS-962212:

BMS-962212 関連抗体

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製品説明

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[1].

体外実験

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.

BMS-962212 関連抗体
Parmacokinetics
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
体内実験

BMS-962212 (single bolus 0.23-0.46 mg/kg; continuous infusion 1.55-3.1 mg/kg/h; i.v.) inhibits arteriovenous shunt thrombosis in rabbits by up to 83% at the dose of 0.23 mg/kg single bolus combined with 1.55 mg/kg/h continuous infusion[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rabbit[1]
Dosage: 0.23 mg/kg (bolus) + 1.55 mg/kg/h (infusion); 0.46 mg/kg (bolus) + 3.1 mg/kg/h (infusion)
Administration: i.v. bolus; i.v. infusion
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.).
臨床実験
分子量

659.07

分子式

C32H28ClFN8O5
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5173 mL 7.5864 mL 15.1729 mL
5 mM 0.3035 mL 1.5173 mL 3.0346 mL
10 mM 0.1517 mL 0.7586 mL 1.5173 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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体積 （開始）

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体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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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BMS-962212 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-9622121430114-34-3BMS962212BMS 962212Factor XaFxarabbit FXIahuman FXIahuman liver microsomesFactor XIarat liver microsomesrabbit activated plasma kallikreinantithrombotic agenthuman plasmathrombosisdog liver microsomesInhibitorinhibitorinhibit

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