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Product details

名称

H4R antagonist 1

分子类型

未知

别名

H4R 拮抗剂 1

英文名称

H4R antagonist 1

货号

H649780-5mg

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

H4R antagonist 1 is a potent and highly selective histamine H4 receptor ( H4R ) antagonist with an IC 50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R In Vitro The competitive binding assay against a wider panel of GPCR, ion channel, and transporters at the concentration of 10 μM reveals that H4R antagonist 1 (Compound 48) is highly selective for H4R. The inhibitory activity of H4R antagonist 1 against mouse H4R (IC 50 =0.29 μM) is about 10 times weaker than that for human H4R. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD) . In the [ 35 S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC 50 of 0.69 μM . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Human H 4 Receptor 27 nM (IC 50 ) Mouse H 4 Receptor 290 nM (IC 50 )

生化机理

H4R 拮抗剂 1 是一种强效、高选择性的组胺 H4 受体（H4R）拮抗剂，其 IC 50 为 27 nM。H4R 拮抗剂 1 与组胺受体的其他亚型（H1R、H2R 和 H3R）没有明显的结合亲和力。

CAS号

1429375-54-1

分子式

C11H11BrN8

分子量

335.16 g/mol

PubChem编号

71548412

Isomeric SMILES

CNC1CN(C1)C2=NC3=C(C=C(C=N3)Br)N4C2=NN=N4

IIUPAC Name

1-(12-bromo-2,3,4,5,8,10-hexazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-7-yl)-N-methylazetidin-3-amine

INCHI

1S/C11H11BrN8/c1-13-7-4-19(5-7)10-11-16-17-18-20(11)8-2-6(12)3-14-9(8)15-10/h2-3,7,13H,4-5H2,1H3

InChi Key

ICGICUHMULRYIQ-UHFFFAOYSA-N

Smiles

CNC1CN(C1)C2=NC3=C(C=C(C=N3)Br)N4C2=NN=N4

PubChem CID

71548412

溶解性

DMSO : 20 mg/mL (59.67 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

334.029 Da

单同位素质量Monoisotopic Mass

334.029 Da

拓扑极表面积Topological Polar Surface Area

84.100 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

364

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

0.5

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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