1046447-90-8
1046447-90-8 structure
- Name: jnj39758979
- Chemical Name: JNJ-39758979
- CAS Number: 1046447-90-8
- Molecular Formula: C11H19N5
- Molecular Weight: 221.302
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2018-05-30 10:49:33
- Modify Date: 2024-01-02 14:57:58
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JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.
| Name | JNJ-39758979 |
|---|---|
| Synonyms |
4-[(3R)-3-Amino-1-pyrrolidinyl]-6-isopropyl-2-pyrimidinamine
2-Pyrimidinamine, 4-[(3R)-3-amino-1-pyrrolidinyl]-6-(1-methylethyl)- JNJ-39758979 5RV7T5BNMG MFCD28502028 |
| Description | JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. |
|---|---|
| Related Catalog | |
| Target |
Ki: 12.5 nM (histamine H4 receptor)[1] |
| In Vitro | JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. The affinity of JNJ-39758979 for the rat (Ki=188 nM) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 has little if any affinity for the dog H4R (Ki≥10 μM). JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes[1]. |
| In Vivo | JNJ-39758979 shows dose-proportional pharmacokinetic (PK) in rat in the range of 2 to 500 mpK. JNJ-39758979 rapidly reaches the kidneys and liver (mean tmax=2.0 h). The elimination of JNJ-39758979 is slow from the brain, liver, and kidneys, with mean t1/2 values of 42.5, 22.3, and 20.5 h, respectively. The highest exposure (based on Cmax and AUC0-inf values) is observed in the liver followed by the kidney and brain. Tissue-to-plasma ratios for liver and kidney range from 23.2 to 95.8; the tissue-to-plasma ratios in brain increases with time from 0.256 to 22.7 up to 48 h after dosing. JNJ-39758979 is able to inhibit histamine-induced itch at doses of 5 and 20 mg/kg in mice. JNJ-39758979 exhibits dose-dependent inhibition of the clinical score in a mouse collagen-induced arthritis model[1]. |
| Animal Admin | The model of histamine-induced scratching in C57/bl6 mice (n=6 to 8 per group) is used to judge the antipruritic effects of JNJ-39758979. JNJ-39758979 is given p.o. in 20% hydroxypropyl-β-cyclodextran 30 min before an intradermal injection of histamine (100 μg). Bouts of scratching are calculated using an automated system. Immediately after histamine injection, mice are placed in containers above a solenoid, and magnets previously placed on the mouse ear generate scratch-specific signals that are counted over a 20 min time span[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 439.6±55.0 °C at 760 mmHg |
| Molecular Formula | C11H19N5 |
| Molecular Weight | 221.302 |
| Flash Point | 219.6±31.5 °C |
| Exact Mass | 221.164047 |
| LogP | -0.18 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.594 |
| Storage condition | 2-8℃ |