Art. -Nr.: HY-117290

BMS-962212

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BMS-962212 is a factor XIa (FXIa) inhibitor with a K_i of 0.7 nM against human FXIa and a K_i 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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Reinheit: 99.33%
CAS. Nr.: 1430114-34-3
Formel: C₃₂H₂₈ClFN₈O₅
Molecular Weight:659.07

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BMS-962212 Chemical Structure

CAS. Nr.: 1430114-34-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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 K_i of 1100 nM^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_ss	AUC_all	T_1/2
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

In Vivo

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.).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1430114-34-3
Appearance Solid
Molecular Weight 659.07
Formel C₃₂H₂₈ClFN₈O₅
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pinto DJP, et al. Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212). J Med Chem. 2017;60(23):9703-9723. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Clinical Compound Library Plus

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-962212

MCE Bioactive Compound Library

Clinical Compound Library Plus

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-962212 Related Classifications

HY-117290 Related Classifications