1046447-90-8
Chemical Structure
JNJ-39758979
- CAS No.: 1046447-90-8
- Formula:C11H19N5
- Molecular Weight:221.31
IUPAC Name: (R)-4-(3-aminopyrrolidin-1-yl)-6-isopropylpyrimidin-2-amine
InChIKey: COOGVHJHSCBOQT-MRVPVSSYSA-N
SMILES: NC1=NC(C(C)C)=CC(N2C[C@H](N)CC2)=N1
Biological Activity: JNJ-39758979, a chemical probe, 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[1][2].
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JNJ-39758979 | 98.75% | JNJ-39758979, a chemical probe, 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. | ||||||||||||||||||||
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JNJ-39758979 (Standard) | ≥98% | JNJ-39758979 (Standard) is the analytical standard of JNJ-39758979 (HY-101189). This product is intended for research and analytical applications. JNJ-39758979, a chemical probe, 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. | ||||||||||||||||||||
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References
- [1]. Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39. [Content Brief]
- [2]. Murata Y, et al. 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. [Content Brief]
