| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L422197-1ml |
1ml |
现货  |
|
| 别名 | 兰拉普利尼 (GS-9876) |
|---|---|
| 英文别名 |
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] |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Lanraplenib (GS-9876) |
| 生化机理 | 兰雷普尼（GS-9876，GS-SYK）是一种强效、高选择性和口服活性的脾酪氨酸激酶（SYK）抑制剂，其 IC50 值为 9.5 nM。Lanraplenib 通过糖蛋白 VI (GPVI) 受体抑制血小板中 SYK 的活性，不会延长猴子或人类的出血时间 (BT)。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 脾脏相关酪氨酸激酶抑制剂 |
| 产品介绍 |
Lanraplenib (GS-9876, GS-SYK) 是一种有效的、高选择性的 Spleen Tyrosine Kinase (SYK) 的口服活性抑制剂，其IC50值为9.5 nM。Lanraplenib 通过 glycoprotein VI (GPVI) receptor 抑制血小板中的SYK活性，而不会延长猴子或人类的出血时间(BT)。 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 |
| ALogP | 1.211 |
|---|---|
| hba_count | 5 |
| HBD Count | 2 |
| Rotatable Bond | 5 |
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 6-(6-aminopyrazin-2-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine |
| INCHI | 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) |
| InChi Key | XCIGZBVOUQVIPI-UHFFFAOYSA-N |
| Canonical SMILES | C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N |
| Isomeric SMILES | C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N |
| 关联CAS | 1800046-95-0 |
| 分子量 | 443.5 |
| Reaxy-Rn | 28256258 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28256258&ln= |
| DMSO(mg / mL) Max Solubility | 89 |
|---|---|
| DMSO(mM) Max Solubility | 200.676437429538 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 443.500 g/mol |
| XLogP3 | 1.400 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 9 |
| 可旋转键计数Rotatable Bond Count | 5 |
| 精确质量Exact Mass | 443.218 Da |
| 单同位素质量Monoisotopic Mass | 443.218 Da |
| 拓扑极表面积Topological Polar Surface Area | 110.000 Ų |
| 重原子数Heavy Atom Count | 33 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 635.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Reaxy-Rn | 28256258 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28256258&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
首页
400-620-6333
