Nampt-IN-1

≥99%

CAS编号: 1698878-14-6
分子式: C₂₀H₂₅N₃O₅S
分子量: 419.49
PubChem编号: 92044379

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货号 (SKU)	包装规格	是否现货
N648149-5mg	5mg	期货
N648149-10mg	10mg	期货
N648149-25mg	25mg	期货
N648149-50mg	50mg	期货
N648149-100mg	100mg	期货

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Metabolic Enzyme/Protease (4884) NAMPT (29)

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基本描述

规格或纯度	≥99%
英文名称	Nampt-IN-1
生化机理	Nampt-IN-1（LSN3154567）是一种强效的选择性 NAMPT 抑制剂。Nampt-IN-1 可抑制纯化的 NAMPT，其 IC 50 为 3.1 nM。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC 50 of 3.1 nM. In Vitro To assess its selectivity, specificity, and effects on cellular NAD + levels, LSN3154567 is characterized in various biochemical and cellular assays. LSN3154567 inhibits purified NAMPT with an IC 50 of 3.1 nM. When tested against a panel of human kinases (>100; CEREP Kinase panel), it does not exhibit any significant activity (i.e.: IC 50 ≥1 μM) against the kinases tested except CSF1R (IC 50 ≈0.84 μM). LSN3154567 exhibits a broad spectrum of anticancer activity. To assess its anticancer activity, LSN3154567 is tested against a number of different types of cancer cell lines cultured in the absence or presence of nicotinic acid (NA) (10 μM). LSN3154567 exhibits a potent antiproliferative activity against many cell lines in the absence of NA. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Nampt-IN-1 (LSN3154567) exhibits good physical chemical properties that allow oral dosing. When dosed orally with 2 mg/kg in mice, it has an exposure of 195 nMhour in the plasma with a peak concentration of 57 nM (at 0.25 hour) and an oral bioavailability of 39%. When dosed intravenously with 2 mg/kg, it has a hepatic clearance of 158.73 mL/min/kg and a volume of distribution at 7.1 L/kg. The half-life of terminal elimination is estimated to be 2.76 hours. LSN3154567 exhibits a dose-dependent inhibition of NAD + formation with estimated TED 50 value of 2.0 mg/kg. To assess whether LSN3154567 causes retinopathy, rats are treated with LSN3154567 at 20, 40, and 80 mg/kg for 4 days. No apparent retinopathy is observed. The hematological toxicities are observed. When LSN3154567 is dosed at 20, 40, and 80 mg/kg, the plasma exposures obtained are 8,974, 18,061, and 38,327 Mh, respectively. Thus, LSN3154567 exhibits exposure multiples of respective 3-, 7-, and 14-fold over the exposure (2,701 Mh) required for robust efficacy (≈103%) without NA coadministration. Dogs are treated with LSN3154567 at 1 and 2.5 mg/kg. At these dose levels, the retinal toxicity is observed. Degeneration of the outer nuclear layer occurred in all four animals, but is less pronounced in the animals treated with 1 mg/kg. At the 1 and 2.5 mg/kg dose levels, the plasma exposures are determined to be 1,483 and 2,468 nMh, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 3.1 nM (NAMPT), 0.84 μM (CSF1R)

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作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IUPAC Name	2-hydroxy-2-methyl-N-[2-(2-pyridin-3-yloxyacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]propane-1-sulfonamide
INCHI	InChI=1S/C20H25N3O5S/c1-20(2,25)14-29(26,27)22-17-6-5-16-12-23(9-7-15(16)10-17)19(24)13-28-18-4-3-8-21-11-18/h3-6,8,10-11,22,25H,7,9,12-14H2,1-2H3
InChi Key	QHHSCLARESIWBH-UHFFFAOYSA-N
Canonical SMILES	CC(C)(CS(=O)(=O)NC1=CC2=C(CN(CC2)C(=O)COC3=CN=CC=C3)C=C1)O
Isomeric SMILES	CC(C)(CS(=O)(=O)NC1=CC2=C(CN(CC2)C(=O)COC3=CN=CC=C3)C=C1)O
PubChem CID	92044379
分子量	419.49

化学和物理性质

溶解性	DMSO : 250 mg/mL (595.96 mM; Need ultrasonic)
分子量	419.500 g/mol
XLogP3	1.300
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	7
可旋转键计数Rotatable Bond Count	7
精确质量Exact Mass	419.151 Da
单同位素质量Monoisotopic Mass	419.151 Da
拓扑极表面积Topological Polar Surface Area	117.000 Å²
重原子数Heavy Atom Count	29
形式电荷Formal Charge	0
复杂度Complexity	664.000
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

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Nampt-IN-1

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基本描述

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关联靶点（其它种属）

作用机制

名称和识别符

化学和物理性质

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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