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jnj39758979 - 97%, high purity , CAS No.1046447-90-8, Antagonist of H 1 receptor;Antagonist of H 2 receptor;Antagonist of H 3 receptor;Antagonist of H 4 receptor

  • Moligand™
  • ≥97%
Item Number
J171811
Grouped product items
SKUSizeAvailabilityPrice Qty
J171811-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$69.90
J171811-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$189.90
J171811-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$299.90
J171811-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$499.90
J171811-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$699.90
J171811-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$999.90

Basic Description

SynonymsJNJ-39758979|1046447-90-8|jnj39758979|JNJ 39758979|4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylpyrimidin-2-amine|5RV7T5BNMG|CHEMBL3236549|4-[(3R)-3-aminopyrrolidin-1-yl]-6-(propan-2-yl)pyrimidin-2-amine|2-Pyrimidinamine, 4-((3R)-3-amino-1-pyrrolidinyl)-6
Specifications & PurityMoligand™, ≥97%
Storage TempStore at 2-8°C,Protected from light
Shipped InWet ice
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of H 1 receptor;Antagonist of H 2 receptor;Antagonist of H 3 receptor;Antagonist of H 4 receptor
Product Description

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.

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GGT6 Tbio Glutathione hydrolase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EPHA1 Tchem Ephrin type-A receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR7 Tclin 5-hydroxytryptamine receptor 7 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALK Tclin ALK tyrosine kinase receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR6 Tchem 5-hydroxytryptamine receptor 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK2 Tchem Serine/threonine-protein kinase Chk2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EDNRA Tclin Endothelin-1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylpyrimidin-2-amine
INCHI 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
Canonical 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
Alternate CAS 1046447-90-8
PubChem CID 24994634
MeSH Entry Terms 4-(3-aminopyrrolidin-1-yl)-6-isopropylpyrimidin-2-ylamine;JNJ 39758979
Molecular Weight 221.30

Certificates

Certificate of Analysis(COA)

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12 results found

Lot NumberCertificate TypeDateItem
H2428205Certificate of AnalysisMay 18, 2024 J171811
H2428206Certificate of AnalysisMay 18, 2024 J171811
H2428207Certificate of AnalysisMay 18, 2024 J171811
H2428208Certificate of AnalysisMay 18, 2024 J171811
H2428209Certificate of AnalysisMay 18, 2024 J171811
H2428214Certificate of AnalysisMay 18, 2024 J171811
H2428215Certificate of AnalysisMay 18, 2024 J171811
H2428216Certificate of AnalysisMay 18, 2024 J171811
H2428217Certificate of AnalysisMay 18, 2024 J171811
H2428218Certificate of AnalysisMay 18, 2024 J171811
H2428219Certificate of AnalysisMay 18, 2024 J171811
H2428220Certificate of AnalysisMay 18, 2024 J171811

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Chemical and Physical Properties

SensitivityLight sensitive

Related Documents

References

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]

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