UR-PI376
| Code | Size | Price |
|---|
| TAR-T35003-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T35003-50mg | 50mg | £1,661.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T35003-100mg | 100mg | £2,079.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
UR-PI376 is a histamine H4 receptor agonist (hH4R agonist) (pEC50 = 7.47, alpha = 0.93), with low activity for hH1R and hH2R and significant selectivity for hH3R (pKB = 6.00, alpha =- 0.28), as in stable-use a membrane preparation of hH(x)R-expressing Sf9 cells for state GTPase detection.
CAS:
1192559-94-6
Formula:
C17H22N6S
Molecular Weight:
342.47
Purity:
0.98
SMILES:
N#CNC(NCCSc1ccccc1)=N/CCCCc1cnc[nH]1
References
Werner K, Neumann D, Buschauer A, Seifert R. No evidence for histamine H4 receptor in human monocytes. J Pharmacol Exp Ther. 2014 Dec;351(3):519-26. doi: 10.1124/jpet.114.218107. Epub 2014 Oct 1. PubMed PMID: 25273276.
Gschwandtner M, Koether B, Werfel T, Stark H, Gutzmer R. Profiling of histamine H4 receptor agonists in native human monocytes. Br J Pharmacol. 2013 Sep;170(1):136-43. doi: 10.1111/bph.12237. PubMed PMID: 23638754; PubMed Central PMCID: PMC3764855.
Geyer R, Nordemann U, Strasser A, Wittmann HJ, Buschauer A. Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H(4) Receptor Agonists. J Med Chem. 2016 Apr 5. [Epub ahead of print] PubMed PMID: 27007611.
Wifling D, Bernhardt G, Dove S, Buschauer A. The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity. PLoS One. 2015 Jan 28;10(1):e0117185. doi: 10.1371/journal.pone.0117185. eCollection 2015. Erratum in: PLoS One. 2015;10(3):e0122162. PubMed PMID: 25629160; PubMed Central PMCID: PMC4309601.