This is a demo store. No orders will be fulfilled.

首页   400-620-6333
  • 登录
  • 注册
  • 英文站
切换导航
我的购物车
搜索
高级搜索
菜单
登录
设置
྾

JNJ39758979,组胺H4受体拮抗剂, H 1 受体拮抗剂；H 2 受体拮抗剂；H 3 受体拮抗剂；H 4 受体拮抗剂

COA COA
有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
J171811-1mg
 1mg 现货 Stock Image
J171811-5mg
 5mg 现货 Stock Image
J171811-10mg
 10mg 现货 Stock Image
J171811-25mg
 25mg 现货 Stock Image
J171811-50mg
 50mg 现货 Stock Image
J171811-100mg
 100mg 现货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
查看相关系列
Class A GPCR (8201) GPCR/G Protein (3179) H1 receptor Antagonist (64) H2 receptor Antagonist (15) H3 receptor Antagonist (29) H4 receptor Antagonist (16) Histamine Receptor (192) Immunology/Inflammation (1938) 神经元信号传导 (3320)
main product photo

基本描述

英文别名 WRB44790 | 5RV7T5BNMG | BDBM50006789 | jnj39758979 | JNJ-39758979 | GTPL8984 | JNJ-39758979, (-)- | 1046447-90-8 | (r)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylamine | Q27888282 | SCHEMBL604514 | 4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylp
规格或纯度 Moligand™, ≥97%
英文名称 jnj39758979
储存温度 2-8°C储存,避光
运输条件 冰袋运输
作用类型 拮抗剂
作用机制 H 1 受体拮抗剂；H 2 受体拮抗剂；H 3 受体拮抗剂；H 4 受体拮抗剂
产品介绍

JNJ-39758979是一种选择性的、具有口服活性的、高亲和力的组胺 H4 受体 (histamine H4 receptor) 拮抗剂，对人，小鼠，猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。JNJ-39758979 对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。JNJ-39758979 具有良好的抗炎、止痒作用。

JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.

纯度 ≥97%

关联靶点（人）

HRH4 Tchem 组胺 H4 受体(Histamine H4 receptor) (5 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)
HRH3 Tclin 组胺 H3 受体(Histamine H3 receptor) (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)
HRH2 Tclin 组胺 H2 受体(Histamine H2 receptor) (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)
HRH1 Tclin 组胺 H1 受体(Histamine H1 receptor) (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)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 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
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRL1 Tchem Nociceptin receptor (3823 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TACR2 Tchem Neurokinin 2 receptor (3341 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NPY2R Tchem Neuropeptide Y receptor type 2 (3731 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CCR1 Tchem C-C chemokine receptor type 1 (1730 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR5A Tchem Serotonin 5a (5-HT5a) receptor (1433 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR6 Tchem Serotonin 6 (5-HT6) receptor (9749 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CXCR2 Tchem Interleukin-8 receptor B (3491 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 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）

Htr7 Serotonin 7 (5-HT7) receptor (19 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hrh4 Histamine H4 receptor (388 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ntsr1 Neurotensin receptor 1 (48 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Salmonella typhimurium (15756 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 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
Kidney (1278 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver microsome (341 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 4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylpyrimidin-2-amine
INCHI 1S/C11H19N5/c1-7(2)9-5-10(15-11(13)14-9)16-4-3-8(12)6-16/h5,7-8H,3-4,6,12H2,1-2H3,(H2,13,14,15)/t8-/m1/s1
InChi Key COOGVHJHSCBOQT-MRVPVSSYSA-N
Smiles CC(C)C1=CC(=NC(=N1)N)N2CCC(C2)N
Isomeric SMILES CC(C)C1=CC(=NC(=N1)N)N2CC[C@H](C2)N
关联CAS 1046447-90-8
MeSH Entry Terms 4-(3-aminopyrrolidin-1-yl)-6-isopropylpyrimidin-2-ylamine;JNJ 39758979
分子量 221.30
Reaxy-Rn 46171385
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=46171385&ln=

化学和物理性质

敏感性 对光线敏感
分子量 221.300 g/mol
XLogP3 0.700
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 5
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 221.164 Da
单同位素质量Monoisotopic Mass 221.164 Da
拓扑极表面积Topological Polar Surface Area 81.100 Ų
重原子数Heavy Atom Count 16
形式电荷Formal Charge 0
复杂度Complexity 232.000
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 1
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

安全和危险性（GHS）

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:

通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！

找到12个结果

批号(Lot Number) 证书类型 货号
H2428206 分析证书 J171811
H2428207 分析证书 J171811
H2428218 分析证书 J171811
H2428219 分析证书 J171811
H2428205 分析证书 J171811
H2428208 分析证书 J171811
H2428209 分析证书 J171811
H2428214 分析证书 J171811
H2428217 分析证书 J171811
H2428220 分析证书 J171811
H2428215 分析证书 J171811
H2428216 分析证书 J171811

显示更多⌵

引用文献

1. Savall BM, Chavez F, Tays K, Dunford PJ, Cowden JM, Hack MD, Wolin RL, Thurmond RL, Edwards JP.  (2014)  Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists..  J Med Chem,  57  (6): (2429-39).  [PMID:24495018]
2. Thurmond RL, Chen B, Dunford PJ, Greenspan AJ, Karlsson L, La D, Ward P, Xu XL.  (2014)  Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979..  J Pharmacol Exp Ther,  349  (2): (176-84).  [PMID:24549371]
3. Kollmeier A, Francke K, Chen B, Dunford PJ, Greenspan AJ, Xia Y, Xu XL, Zhou B, Thurmond RL.  (2014)  The histamine H₄ receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects..  J Pharmacol Exp Ther,  350  (1): (181-7).  [PMID:24817035]
4. Murata Y, Song M, Kikuchi H, Hisamichi K, Xu XL, Greenspan A, Kato M, Chiou CF, Kato T, Guzzo C et al..  (2015)  Phase 2a, randomized, double-blind, placebo-controlled, multicenter, parallel-group study of a H4 R-antagonist (JNJ-39758979) in Japanese adults with moderate atopic dermatitis..  J Dermatol,  42  (2): (129-39).  [PMID:25491792]

溶液计算器

上海阿拉丁生化科技股份有限公司
© 2016 ALADDIN-E.COM . 版权所有,未经授权禁止拷贝本站资料,如有违反,将追究法律责任

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用。

上海工商 危险品化学品经营许可证（带存储）营业执照(三证合一)