INVA8001
INVA8001 (ASB17061) is a highly selective and orally active chymase inhibitor with IC50 values for human chymase and mouse mast cell proteinase 4 (mMCP-4) of 0.02 and 0.03 μM, respectively. INVA8001 exhibits IC50 values for bovine α-chymotrypsin and human cathesin G of 3.4 and 32.1 μM, respectively, and it shows over 1000-fold selectivity for other related serine proteases. INVA8001 inhibits mast cells in a mouse primary sclerosing cholangitis (PSC) model, improves bile duct pathology, and alleviates bile stasis, demonstrating anti-inflammatory and anti-fibrotic effects.
For research use only. We do not sell to patients.
- CAS No.: 1312993-34-2
- Formula: C29H38ClN5O8
- Molecular Weight:620.09
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1312993-34-2
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Molecular Weight 620.09
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Formula C29H38ClN5O8
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SMILES
[H][C@@]1(CN/C(CN(C1=O)C(N[C@](CCC)(C2=CC=C(C(N)=C2)C(O)=O)[H])=O)=N\OCC)CC3=C(C=CC(Cl)=C3)OC.CC(O)=O
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Synonyms
ASB17061
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
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Protocol for Hematoxylin-Eosin (H&E) Staining
Hematoxylin-eosin staining is a routine histological method that stains nuclei mainly blue-purple with hemalum and stains cytoplasm, extracellular matrix, and many stromal components pink with eosin, allowing tissue architecture, cell morphology, necrosis, inflammation, fibrosis, tumor growth pattern, and treatment-associated injury to be evaluated by light microscopy. In cancer cells, primary neurons, mouse tumor models, intestinal organoids, inflammatory macrophage preparations, and drug-screening tissues, H&E is a morphology assay rather than a molecular assay; it should be interpreted with complementary molecular or immunostaining assays when the biological question concerns specific proteins, RNA levels, ferroptosis, mitophagy, or immune phenotypes.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)