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Cat. No.: HY-151196

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FXIa-IN-10

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an K_i of 0.17 nM. FXIa-IN-10 has good oral bioavailability.

For research use only. We do not sell to patients.

CAS No.: 2816108-08-2
Formula: C₂₃H₁₈Cl₂F₃N₉O₂
Molecular Weight:580.35

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

FXIa-IN-10 Chemical Structure

CAS No.: 2816108-08-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an K_i of 0.17 nM. FXIa-IN-10 has good oral bioavailability^[1].

IC₅₀ & Target

K_i: 0.17 nM (FXIa)^[1]

In Vivo

FXIa-IN-10 (Compound 3f) (1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg; i.v.; twice) shows antithrombotic efficacy in a rabbit AV shunt thrombosis model^[1].
FXIa-IN-10 (0-10 mg/kg; p.o.; once) demonstrates oral bioavailability in preclinical species (rat 36.4%, dog 80.5%, and monkey 43.0%)^[1].

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

Animal Model:

Male New Zealand White (NZW) rabbits, AV shunt thrombosis model^[1]
Dosage:

1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg
Administration:

Intravenous injection, 20 min prior to and 40 min during the AV shunt
Result:

Reduced thrombus weights in a dose-dependent manner.

Animal Model:

Sprague-Dawley rats, Beagle dogs, Cynomolgus monkeys^[1]
Dosage:

1, 2, 5 or 10 mg/kg
Administration:

Intravenous or oral administration (Pharmacokinetic Analysis)

Result:

Pharmacokinetic Profile of FXIa-IN-10 (Compound 3f) in Preclinical Species^a^[1]

animal species	clearance (mL/min/kg)	T_1/2 (h)	V_dss (L/kg)	F%	AUC (iv) (μM•h)	AUC (po) (μM•h)	Dose iv/po (mpk)
rat	10.7 ± 1.8	1.4 ± 0.0	0.8 ± 0.1	36.4	5.5 ± 1.0	10.0 ± 2.4	2/10
monkey	25.6 ± 4.0	1.0 ± 0.4	1.5 ± 0.4	43.0	1.1 ± 0.2	2.5 ± 0.3	1/5

^aCompound was dosed as a free base, vehicle for iv: 20% HPbCD and po: 10% ethanol; 70% PEG-400; 20% water. Data were derived from three animals per study.

Chemical Information

CAS No. 2816108-08-2
Molecular Weight 580.35
Formula C₂₃H₁₈Cl₂F₃N₉O₂
SMILES

CN1N=NC=C1C2=CN([C@@H](C3=CC=C(C4=C(N5N=NC(Cl)=C5)C=CC(Cl)=C4F)C=[N+]3[O-])CCOC(F)F)N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)

References

[1]. Xu G, et al. Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions. J Med Chem. 2022 Aug 11;65(15):10419-10440. [Content Brief]

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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.

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