FXIa-IN-10
FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki 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.
Biological Activity
Description
IC50 & Target
Ki: 0.17 nM (FXIa)[1]
In Vivo
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 Speciesa[1]
animal species clearance (mL/min/kg) T1/2 (h) Vdss (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.
Protocols
-
Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)