Perforin-IN-1
Perforin-IN-1 is a perforin inhibitor that blocks perforin-mediated lysis of target cells by cytotoxic lymphocytes. Perforin-IN-1 achieves perforin inhibition in a mouse bone marrow transplantation model, protecting MHC-mismatched allogeneic bone marrow stem cell grafts from NK cell-mediated rejection. Perforin-IN-1 can be used for research on graft rejection.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2378640-25-4
- Formule: C24H18F2N4O4S2
- Masse moléculaire:528.55
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
3.34 μM
|
Inhibition of purified recombinant perforin-mediated lysis of Jurkat T lymphoma target cells measured by 51Cr release after 4 hrs incubation.
Inhibition of purified recombinant perforin-mediated lysis of Jurkat T lymphoma target cells measured by 51Cr release after 4 hrs incubation.
|
31525966 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Jurkat T lymphoma cells
-
Concentration:20, 10, 5, 2.5, and 1.25 μM
-
Incubation Time:30 min preincubation with recombinant perforin; 4 h incubation
-
Result:Inhibited purified recombinant perforin-mediated lysis of Jurkat T lymphoma cells with an IC50 of 3.34 μM.
-
Cell Line:KHYG-1 NK cells
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:KHYG-1 NK cell viability was 90.6% at 10 μM.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-∞ |
|---|---|---|---|---|
| Mice[1] | 90 mg/kg | i.p. | 18.9 h | 42475 μM/L·h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (wild-type recipients; donor bone marrow from BALB/c and B6.SJL-Ptprca mice (mixed at a 1:1 ratio, 24 × 106 cells total))[1]
-
Dosage:125 mg/kg
-
Administration:i.p.; at 0 h immediately before cell transfer and at 18 h after cell transfer
-
Result:Demonstrated a 66% reduction of perforin activity, resulting in preservation of transplanted mismatched target cells.
In comparison to perforin knockout recipients, representing 100% perforin inhibition, a 66% reduction in perforin activity was observed as measured by survival of the transferred allogeneic cells.
Chemical Information
-
CAS No. 2378640-25-4
-
Masse moléculaire 528.55
-
Formule C24H18F2N4O4S2
-
SMILES
FC1=CC(F)=CC=C1S(NC2=C(OC)N=CC(C3=CC=C(C4=CN=C(C(N(C)C5)=O)C5=C4)S3)=C2)(=O)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Perforin-IN-1 Related Classifications
HY-129387 Related Classifications
Powered by Bioz