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].
For research use only. We do not sell to patients.
- CAS No.: 2744293-04-5
- Formula: C31H29ClN8O5
- Molecular Weight:629.07
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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 No. 2744293-04-5
-
Molecular Weight 629.07
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FXIa-IN-8 Related Classifications
HY-144658 Related Classifications
Powered by Bioz