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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
Lanraplenib (GS-9876) - Moligand™, ≥98% , Inhibitor of spleen associated tyrosine kinase, CAS No.1800046-95-0, Inhibitor of spleen associated tyrosine kinase
Disponible para pedir
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. ≥98%
Synonyms
DB14770 | Lanraplenib (GS-9876) | AC-36571 | InChI=1/C3H6ClNO2/c4-1-2(5)3(6)7/h2H,1,5H2,(H,6,7)/t2-/m0/s1 | EX-A3747 | XCIGZBVOUQVIPI-UHFFFAOYSA-N | 6-(6-amino-2-pyrazinyl)-N-[4-[4-(3-oxetanyl)-1-piperazinyl]phenyl]-imidazo[1,2-a]
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
Why this grade
Moligand™, ≥98% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
Targets
GPVI receptor ; Syk (Cell-free assay) ; 9.5 nM
In vitro
GS-9876 inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC50 values of 24–51 nM. Functionally, GS-9876 inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC50=112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC50=108±55 nM). In human macrophages, GS-9876 inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively). Anti-CD3/anti-CD28 stimulated T cell proliferation is weakly inhibited (EC50=1291±398 nM), with selectivity >10-fold versus the inhibition of B cell proliferation. In human blood, GS-9876 blocks SYK phosphorylation, CD69 expression on B cells, and CD63 expression in basophils.\xa0GS-9876 inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow.
In vivo
GS-9876 demonstrates a dose-dependent improvement in clinical score and histopathology parameters with once-daily dosing in short and long term rat models of collagen-induced arthritis (CIA). Significant efficacy can be achieved with GS-9876 doses that produces trough pSYK inhibition of <50%. Ex vivo, GPVI-stimulated platelet aggregation is inhibited in GS-9876-treated monkeys without a concomitant increase in bleeding time (BT). Similarly, orally administered GS-9876 does not increase BT in humans.
Cell Research(from reference)
Cell lines：Human blood platelets
Concentrations：0.01 μM to 100 μM
Incubation Time：15 min
Specifications
Sinónimos
DB14770 | Lanraplenib (GS-9876) | AC-36571 | InChI=1/C3H6ClNO2/c4-1-2(5)3(6)7/h2H, 1, 5H2, (H, 6, 7)/t2-/m0/s1 | EX-A3747 | XCIGZBVOUQVIPI-UHFFFAOYSA-N | 6-(6-amino-2-pyrazinyl)-N-[4-[4-(3-oxetanyl)-1-piperazinyl]phenyl]-imidazo[1, 2-a]
Especificaciones y pureza
Moligand™, ≥98%
Mecanismos bioquímicos y fisiológicos
Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding
Condiciones de almacenamiento de almacenamiento
Store at -20°C
Enviado en
Ice chest + Ice pads
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of spleen associated tyrosine kinase
Pureza
≥98%
Propiedades del producto
| ALogP | 1.211 |
|---|---|
| hba_count | 5 |
| Recuento HBD | 2 |
| Enlace rotable | 5 |
Nombres e identificadores
| Pubchem Sid | 504772855 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504772855 |
| Sonrisas canónicas | C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N |
| IUPAC Name | 6-(6-aminopyrazin-2-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine |
| InChIKey | XCIGZBVOUQVIPI-UHFFFAOYSA-N |
| INCHI | 1S/C23H25N9O/c24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18/h1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29) |
| Isómeros SMILES | C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N |
| CAS alternativo | 1800046-95-0 |
| Peso molecular | 443.5 |
| Reaxy-Rn | 28256258 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28256258&ln= |
Documentation
📋 Safety Data Sheet (SDS)
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →✅ Certificate of Analysis (COA)
Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →🔬 Specification Sheet
Full quality attributes and acceptance criteria for this grade.
View spec sheet →Advanced Data
Taxonomic Classification
Taxonomy Tree
- Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
- Clase Diazinanes
- Subclass Piperazines
- Clase Diazinanes
- Superclass Organoheterocyclic compounds
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Clase | Diazinanes |
| Subclass | Piperazines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylpiperazines |
| Alternative Parents | N-arylpiperazines Imidazopyrazines Dialkylarylamines Aniline and substituted anilines N-alkylpiperazines Aminopyrazines N-substituted imidazoles Imidolactams Heteroaromatic compounds Trialkylamines Oxetanes Secondary amines Oxacyclic compounds Dialkyl ethers Azacyclic compounds Primary amines Organopnictogen compounds Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | N-arylpiperazine - Phenylpiperazine - Imidazopyrazine - Aniline or substituted anilines - Dialkylarylamine - Tertiary aliphatic/aromatic amine - N-alkylpiperazine - Aminopyrazine - Imidolactam - Benzenoid - Pyrazine - N-substituted imidazole - Monocyclic benzene moiety - Heteroaromatic compound - Imidazole - Azole - Tertiary aliphatic amine - Tertiary amine - Oxetane - Oxacycle - Azacycle - Secondary amine - Ether - Dialkyl ether - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Amine - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group. |
| External Descriptors | Not available |
Estructura 3D
Modelo de Estructura Química Interactiva
Objetivos asociados (humanos)
CD63 Tchem CD63 antigen (1 Activities)
SYK Tclin Tyrosine-protein kinase SYK (5 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
SYK Tclin Tyrosine-protein kinase SYK (7372 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
Objetivos asociados (no humanos)
Mus musculus (284745 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
Mecanismos de acción
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Fecha | Articulo |
|---|---|---|---|
 I2512018 | Certificate of Analysis | Sep 23, 2025 | L414473 |
| I2205064 | Certificate of Analysis | Jun 10, 2025 | L414473 |
| I2205065 | Certificate of Analysis | Jun 10, 2025 | L414473 |
| I2205066 | Certificate of Analysis | Jun 10, 2025 | L414473 |
| I2205067 | Certificate of Analysis | Jun 10, 2025 | L414473 |
| I2205068 | Certificate of Analysis | Jun 10, 2025 | L414473 |
Propiedades químicas y físicas
| Solubilidad | Solubility (25°C) In vitro DMSO: 89 mg/mL (200.67 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| DMSO (mg/ml) Solubilidad máxima | 89 |
| DMSO (mM) Solubilidad máxima | 200.676437429538 |
| Agua (mg/ml) Solubilidad máxima | ＜1 |
| Peso molecular | 443.500 g/mol |
| XLogP3 | 1.400 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 5 |
| Exact Mass | 443.218 Da |
| Monoisotopic Mass | 443.218 Da |
| Topological Polar Surface Area | 110.000 Ų |
| Heavy Atom Count | 33 |
| Formal Charge | 0 |
| Complexity | 635.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
Calculadoras de soluciones
Reseñas
Reseñas de cliente
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