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Nav1.7-IN-3

    级别和纯度:
  • ≥98%
有货

库存信息

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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
N649481-5mg
5mg 期货 Stock Image
N649481-10mg
10mg 期货 Stock Image
N649481-25mg
25mg 期货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 Nav1.7-IN-3
生化机理 Nav1.7-IN-3 是一种选择性口服生物活性电压门控钠通道 Nav1.7 抑制剂,其 IC 50 为 8 nM。止痛。中枢神经系统渗透有限。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC 50 of 8 nM. Pain relief. Limited CNS penetration

In Vivo

Nav1.7-IN-3 (compound 5) shows excellent potency, selectivity, behavioral efficacy in a rodent pain model (30 mg/kg, oral, 35 minutes), and efficacy in a mouse itch model (30 mg/kg, oral, 30 minutes) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 male mice (n=8/group, 25-30g) Dosage: 1, 3, and 10 mg/kg Administration: Oral (0-35 mintues) Result: Nav1.7-IN-3 demonstrates statistically significant, dose-dependent reversal of these effects in the acute phase of the experiment (0-5 min period post formalin injection) and the tonic phase of the experiment (20-35 min period post formalin injection) with full reversal of formalin effects in the tonic phase

Form:Solid

IC50& Target:IC50: 8 nM (Nav1.7)

纯度 ≥98%

关联靶点(人)

SCN5A Tclin 钠通道蛋白 5 型亚基 α(Sodium channel protein type 5 subunit alpha) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SCN9A Tclin 钠通道蛋白 9 型亚基 α(Sodium channel protein type 9 subunit alpha) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SCN8A Tclin 钠通道蛋白 8 型亚基 α(Sodium channel protein type 8 subunit alpha) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1D Tclin Alpha-1d adrenergic receptor (4171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Scn9a Sodium channel protein type IX alpha subunit (69 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn8a Sodium channel protein type VIII alpha subunit (53 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Brain (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn9a Sodium channel protein type 9 subunit alpha (111 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

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
IIUPAC Name 5-chloro-2-fluoro-4-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethylamino)-N-(1,3-thiazol-2-yl)benzenesulfonamide
INCHI 1S/C17H20ClFN4O2S2/c18-12-9-15(27(24,25)22-16-20-5-8-26-16)13(19)10-14(12)21-11-17-3-1-6-23(17)7-2-4-17/h5,8-10,21H,1-4,6-7,11H2,(H,20,22)
InChi Key XFWKBJBSEOZBRA-UHFFFAOYSA-N
Smiles C1CC2(CCCN2C1)CNC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=NC=CS4)F
Isomeric SMILES C1CC2(CCCN2C1)CNC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=NC=CS4)F
PubChem CID 118112300
分子量 430.95

化学和物理性质

溶解性 DMSO : <1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器