JNJ-39758979

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531985

CAS#: 1046447-90-8

Description: JNJ-39758979 is histamine H4 receptor antagonists.

Chemical Structure

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JNJ-39758979
CAS# 1046447-90-8
Instruction

Theoretical Analysis

MedKoo Cat#: 531985
Name: JNJ-39758979
CAS#: 1046447-90-8
Chemical Formula: C11H19N5
Exact Mass: 221.16
Molecular Weight: 221.310
Elemental Analysis: C, 59.70; H, 8.65; N, 31.65

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: JNJ-39758979; JNJ 39758979; JNJ39758979.

IUPAC/Chemical Name: 4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylpyrimidin-2-amine

InChi Key: COOGVHJHSCBOQT-MRVPVSSYSA-N

InChi Code: 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

SMILES Code: NC1=NC(C(C)C)=CC(N2C[C@H](N)CC2)=N1

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 221.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Thurmond RL, Venable J, Savall B, La D, Snook S, Dunford PJ, Edwards JP. Clinical Development of Histamine H(4) Receptor Antagonists. Handb Exp Pharmacol. 2017 Feb 24. doi: 10.1007/164_2016_130. [Epub ahead of print] PubMed PMID: 28233185.

2: Sulaiman I, Lim JC, Soo HL, Stanslas J. Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation. Pulm Pharmacol Ther. 2016 Oct;40:52-68. doi: 10.1016/j.pupt.2016.07.005. Review. PubMed PMID: 27453494.

3: Murata Y, Song M, Kikuchi H, Hisamichi K, Xu XL, Greenspan A, Kato M, Chiou CF, Kato T, Guzzo C, Thurmond RL, Ohtsuki M, Furue M. 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. 2015 Feb;42(2):129-39. doi: 10.1111/1346-8138.12726. PubMed PMID: 25491792.

4: Seifert R. Therapeutic efficacy of a H₄ receptor antagonist in humans: a milestone in histamine research. J Pharmacol Exp Ther. 2014 Jul;350(1):2-4. doi: 10.1124/jpet.114.215749comm. PubMed PMID: 24925898.

5: Kollmeier A, Francke K, Chen B, Dunford PJ, Greenspan AJ, Xia Y, Xu XL, Zhou B, Thurmond RL. 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. 2014 Jul;350(1):181-7. doi: 10.1124/jpet.114.215749. PubMed PMID: 24817035.

6: Thurmond RL, Chen B, Dunford PJ, Greenspan AJ, Karlsson L, La D, Ward P, Xu XL. Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979. J Pharmacol Exp Ther. 2014 May;349(2):176-84. doi: 10.1124/jpet.113.211714. PubMed PMID: 24549371.

7: Savall BM, Chavez F, Tays K, Dunford PJ, Cowden JM, Hack MD, Wolin RL, Thurmond RL, Edwards JP. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39. doi: 10.1021/jm401727m. PubMed PMID: 24495018.