JNJ-39758979 dihydrochloride 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 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity.

Product information

CAS Number: 1620648-30-7

Molecular Weight: 294.22

Formula: C11H21Cl2N5

Chemical Name: (R)-4-(3-aminopyrrolidin-1-yl)-6-isopropylpyrimidin-2-amine dihydrochloride

Smiles: Cl.Cl.CC(C)C1=CC(=NC(N)=N1)N1CC[C@@H](N)C1

InChiKey: KXPWYAVIFCXPRW-YCBDHFTFSA-N

InChi: InChI=1S/C11H19N5.2ClH/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);2*1H/t8-;;/m1../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM versus the human H4 receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H4R, the Ki=5.3 nM and the pA2=8.3. At the monkey H4R, the Ki=25 nM and the pA2=7.5. The affinity for the rat (Ki=188 nM, pA2 = 7.2) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H4R (Ki≥10 μM). The compound is highly selective for H4R, as it exhibits low affinity for the H1, H2, and H3 receptors. JNJ-39758979 dihydrochloride is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes.

In Vivo:

JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 and F values are 0.3 μM, 7.5 hours, 36%, respectively. JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively .

Products are for research use only. Not for human use.