FXIa-IN-8
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2744293-04-5
- Formel: C31H29ClN8O5
- Molecular Weight:629.07
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 14.2 nM (FXIa); 27900 nM (PKal)[1]
In Vitro
FXIa-IN-8 (compound 35) (0-250 µg/mL) shows significant anticoagulant activity toward the intrinsic pathway without affecting the extrinsic pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
FXIa-IN-8 (6.5, 19.5 mg/kg; i.v.) shows antithrombotic activity in vivo[1].
FXIa-IN-8 (50, 100 mg/kg; i.v.) shows no acute toxicity[1].
FXIa-IN-8 (10 mg/kg; i.v.) shows moderate PK profiles[1]. FXIa-IN-8 (19.5, 39 mg/kg) exhibits a much lower bleeding risk than heparin sodium at 300 IU/kg[1].
Pharmacokinetic Parameters of FXIa-IN-8 in Male SD rats[1].
| compd 35 | T1/2 (h) | Cmax (µg/mL) | AUC0-t (h·µg/mL) | AUC0-∞ (h·µg/mL) | Vz(mL/kg) | Cl (mL/h/kg) | MRT0-t (h) |
| i.v. (10 mg/kg) | 1.26 | 57 | 18.3 | 18.4 | 969 | 553 | 0.32 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male SD rats[1]
-
Dosage:10 mg/kg (300 IU/kg (2.7 mg/kg) heparin sodium were injected into the tail vein 10 min before surgery)
-
Administration:I.v.
-
Result:Showed moderate PK profiles with a half-life value (T1/2) of 1.26 h and a clearance (Cl) value of 553 mL/h/kg.
-
Animal Model:C57BL/6J mice (FeCl3-induced carotid artery thrombus model)[1]
-
Dosage:6.5, 19.5 mg/kg
-
Administration:I.v.
-
Result:Slightly prolonged the time of occlusion at 6.5 mg/kg, and showed excellent antithrombotic activity at 35 mg/kg.
-
Animal Model:ICR mice[1]
-
Dosage:50, 100 mg/kg
-
Administration:I.v.
-
Result:Showed no obvious toxic reaction to different tissues of mice.
-
Animal Model:C57BL/6J mice[1]
-
Dosage:19.5, 39, 20, 60, 100 mg/kg
-
Administration:I.v.
-
Result:Showed a low bleeding risk at 60 and 100 mg/kg.
Chemical Information
-
CAS. Nr. 2744293-04-5
-
Molecular Weight 629.07
-
Formel C31H29ClN8O5
-
SMILES
ClC1=CC(/C=C/C(N[C@H](C(NC2=CC=C(C=C2)C(O)=O)=O)CC(N3CCN(CC3)C4=CC=CC=C4)=O)=O)=C(C=C1)N5C=NN=N5
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
FXIa-IN-8 Related Classifications
HY-144658 Related Classifications
Powered by Bioz