NaV1.7 inhibitor-1

Name: NaV1.7 inhibitor-1
Brand: TargetMol
SKU: T12181
Price: 969 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.89%

货号 T12181Cas号 1494585-79-3

NaV1.7 inhibitor-1 是有效的、选择性的电压门控钠通道 (Nav) 1.7 抑制剂，对于hNaV1.7的IC50为 0.6 nM，其选择性是 hNaV1.5 的 80 倍。

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NaV1.7 inhibitor-1

一键复制产品信息

很棒

纯度: 99.89%

货号 T12181Cas号 1494585-79-3

NaV1.7 inhibitor-1 是有效的、选择性的电压门控钠通道 (Nav) 1.7 抑制剂，对于hNaV1.7的IC50为 0.6 nM，其选择性是 hNaV1.5 的 80 倍。

规格	价格	库存
1 mg	¥ 969	现货
5 mg	¥ 2,420	现货
10 mg	¥ 3,880	现货
25 mg	¥ 6,130	现货
50 mg	¥ 8,280	现货
100 mg	¥ 10,900	现货
200 mg	¥ 14,800	现货
1 mL x 10 mM (in DMSO)	¥ 2,320	现货

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产品介绍

NaV1.7 inhibitor-1 AI Summary

NaV1.7 inhibitor-1 is a potent inhibitor of voltage-gated sodium channels (NaV's), especially highlighting significant activity against Nav1.7. The compound demonstrates very low IC50 values ranging from 0.6 to 50.0 nM across several sodium channel subtypes (Nav1.1, Nav1.2, Nav1.5, Nav1.6, and Nav1.7), with selectivity indices emphasizing a strong preference for Nav1.7 compared to others. Specifically, the IC50 for Nav1.7 inhibition is 2.2 nM in mice and 3.7 nM in rats. Furthermore, electrophysiological assays revealed an IC50 of 4.0 nM, while radioligand binding studies indicated an IC50 of 3.0 nM, corroborating its high affinity for sodium channels. In vivo studies illustrate its antinociceptive effects in mouse models of pain and erythromelalgia, reducing nociceptive behavior in a dose-dependent manner. The compound also boasts good oral bioavailability and favorable pharmacokinetics, including a reasonable half-life, clearance, and volume of distribution, with a low unbound fraction in mouse plasma..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).
靶点活性	Nav1.7 (human):0.6 nM

化学信息

分子量	435.55
分子式	C₂₃H₃₀FNO₄S
CAS No.	1494585-79-3
Smiles	CC1(COc2cc(F)c(cc2C2CC2)C(=O)NS(=O)(=O)C2CC2)CCC2(CC2)CC1
密度	1.32 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 90 mg/mL (206.64 mM), Sonication and heating to 60℃ are recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2959 mL	11.4797 mL	22.9595 mL	114.7974 mL
5 mM	0.4592 mL	2.2959 mL	4.5919 mL	22.9595 mL
10 mM	0.2296 mL	1.1480 mL	2.2959 mL	11.4797 mL
20 mM	0.1148 mL	0.5740 mL	1.1480 mL	5.7399 mL
50 mM	0.0459 mL	0.2296 mL	0.4592 mL	2.2959 mL
100 mM	0.0230 mL	0.1148 mL	0.2296 mL	1.1480 mL