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Product details

名称

PF-04856264

分子类型

小分子

英文别名

英文名称

PF-04856264

货号

P646186-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC 50 s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect In Vivo PF-04856264 (3-30 mg/kg; i.p.) reverses OD1-induced pain behaviors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks adult male C57BL/6J mice (OD1-induced spontaneous pain model)Dosage: 3, 30 mg/kg Administration: I.p. Result: Significantly reduced spontaneous pain behaviors in mice. Form:Solid IC50& Target:IC50: 28 (human Nav1.7), 131 nM (mouse Nav1.7), 19 nM (cynomolgus monkey Nav1.7), 42 nM (dog Nav1.7)

生化机理

PF-04856264 是一种强效的选择性 Nav1.7 抑制剂，对人、小鼠、猴和狗 Nav1.7 的 IC 50 s 分别为 28、131、19 和 42 nM。PF-04856264 对大鼠 Nav1.7 通道的效力较低。PF-04856264 具有镇痛作用

CAS号

1235397-05-3

分子式

C20H15N5O3S2

分子量

437.49 g/mol

PubChem编号

71718072

Isomeric SMILES

CN1C(=CC=N1)C2=CC=CC=C2OC3=C(C=C(C=C3)S(=O)(=O)NC4=NC=CS4)C#N

IIUPAC Name

3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide

INCHI

1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)

InChi Key

MKSKJVIBSRUWSZ-UHFFFAOYSA-N

Smiles

CN1C(=CC=N1)C2=CC=CC=C2OC3=C(C=C(C=C3)S(=O)(=O)NC4=NC=CS4)C#N

PubChem CID

71718072

溶解性

DMSO : 250 mg/mL (571.44 mM; ultrasonic and warming and heat to 60°C)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

437.062 Da

单同位素质量Monoisotopic Mass

437.062 Da

拓扑极表面积Topological Polar Surface Area

147.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

736

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

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