2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. FXIIa-IN-6

FXIIa-IN-6 is a potent, selective, and irreversible covalent inhibitor of Factor XIIa (FXIIa) with an IC50 of 2 nM. FXIIa-IN-6 exhibits ≥2,500-fold selectivity over related serine proteases. FXIIa-IN-6 exhibits favorable anticoagulant and anti-inflammatory activities and can be used in sepsis research.

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

FXIIa-IN-6

FXIIa-IN-6 Chemical Structure

CAS No. : 3107571-66-1

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FXIIa-IN-6 Related Antibodies

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Description

FXIIa-IN-6 is a potent, selective, and irreversible covalent inhibitor of Factor XIIa (FXIIa) with an IC50 of 2 nM. FXIIa-IN-6 exhibits ≥2,500-fold selectivity over related serine proteases. FXIIa-IN-6 exhibits favorable anticoagulant and anti-inflammatory activities and can be used in sepsis research[1].

IC50 & TargetHY-184008

Factor XIIa

2 nM (IC50)

Factor XIIa

0.51 nM (Ki)

In Vitro

FXIIa-IN-6 (F38) inhibits recombinant FXIIa activity, with an IC50 of 2 nM[1].
FXIIa-IN-6 exhibits time-dependent FXIIa inhibition with increased inhibitory potency after preincubation, indicating an irreversible inhibition mechanism[1].
FXIIa-IN-6 shows high selectivity over homologous serine proteases, including thrombin, PKal, FXa, FXIa, plasmin, tPA, trypsin and chymotrypsin[1].
LC-MS analysis shows that FXIIa-IN-6 forms a stable covalent adduct with FXIIa, confirming its covalent binding mechanism[1].
FXIIa-IN-6 significantly prolongs human activated partial thromboplastin time (aPTT), with an EC1.5X of 11.4 μM, while showing no significant effect on prothrombin time (PT)[1].
FXIIa-IN-6 (1-20 μM; 12 hours) inhibits IL-6 and IL-1β expression in LPS-stimulated macrophages in a concentration-dependent manner [1].
FXIIa-IN-6 (40 μM, 24 hours) in cytotoxicity experiments has no obvious cytotoxicity against RAW264.7 macrophages and maintains more than 80% cell viability in RAW264.7, HEPG2 and HEK-293T cells[1].
FXIIa-IN-6 irreversibly inhibits FXIIa, with a Ki of 0.51 nM, a kinact of 0.061 min-1, and a kinact/Ki of 0.11740 nM-1 min-1[1].

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

FXIIa-IN-6 Related Antibodies

Cell Viability Assay

Cell Line: RAW264.7
Concentration: 40 μM
Incubation Time: 24h
Result: showd no obvious cytotoxicity against RAW264.7 macrophages and maintained more than 80% cell viability in RAW264.7, HEPG2, and HEK-293T cells[1].

RT-PCR

Cell Line: RAW264.7
Concentration: 1-20 μM
Incubation Time: 12h
Result: inhibited IL-6 and IL-1β expression in LPS-stimulated macrophages in a concentration-dependent manner[1].
Parmacokinetics
Species Dose Route
Mice[1] 20 or 40 mg/kg i.p.
In Vivo

FXIIa-IN-6 (F38) (20 mg/kg or 40 mg/kg; i.p.; single dose; 30 min after LPS (HY-D1056) i.p.) increases survival rates in a dose-dependent manner in LPS-induced septic mice, reduces serum IL-6 and IL-1β levels, and alleviates LPS-induced tissue damage in the heart, liver, spleen, lung, and kidney[1].

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

Animal Model: LPS-induced septic mice
Dosage: 20 mg/kg or 40 mg/kg
Administration: i.p.; single dose; 30 min after LPS (HY-D1056) i.p.
Result: increased survival rates in a dose-dependent manner in LPS-induced septic mice, reduced serum IL-6 and IL-1β levels, and alleviated LPS-induced tissue damage in the heart, liver, spleen, lung, and kidney[1].
Molecular Weight

554.64

Formula

C30H34N8O3
CAS No.
SMILES

O=C(C1=C2C(OCC3(CO2)CC3)=C(C=C1)N4C[C@H](CC4)N(C(C)C)C)N5N=C(N=C5N)C6=CN=C7C=CC=CC7=N6
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
References
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FXIIa-IN-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FXIIa-IN-63107571-66-1Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesFactor XIIa InhibitorFXIIa InhibitorF38LPS-induced sepsistricyclic scaffoldserine proteasecovalent inhibitorsInhibitorinhibitorinhibit

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HY-184008
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