Synonym
GSK334429; GSK 334429; GSK-334429.
IUPAC/Chemical Name
(4-propan-2-yl-1,4-diazepan-1-yl)-[1-[6-(trifluoromethyl)pyridin-3-yl]piperidin-4-yl]methanone
InChi Key
AHHPKVQYHXNBQN-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H29F3N4O/c1-15(2)25-8-3-9-27(13-12-25)19(28)16-6-10-26(11-7-16)17-4-5-18(24-14-17)20(21,22)23/h4-5,14-16H,3,6-13H2,1-2H3
SMILES Code
O=C(N1CCN(C(C)C)CCC1)C2CCN(C3=CC=C(C(F)(F)F)N=C3)CC2
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
398.47
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.
| 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 |
1: Kyriakidis K, Zampeli E, Palaiologou M, Tiniakos D, Tiligada E. Histamine H3 and H4 receptor ligands modify vascular histamine levels in normal and arthritic large blood vessels in vivo. Inflammation. 2015;38(3):949-58. doi: 10.1007/s10753-014-0057-1. PubMed PMID: 25359709.
2: Nirogi R, Kandikere V, Bhyrapuneni G, Muddana N, Saralaya R, Ponnamaneni RK, Manoharan AK. In vivo receptor occupancy assay of histamine H₃ receptor antagonist in rats using non-radiolabeled tracer. J Pharmacol Toxicol Methods. 2012 May-Jun;65(3):115-21. doi: 10.1016/j.vascn.2012.03.003. PubMed PMID: 22487318.
3: Medhurst SJ, Collins SD, Billinton A, Bingham S, Dalziel RG, Brass A, Roberts JC, Medhurst AD, Chessell IP. Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. Pain. 2008 Aug 15;138(1):61-9. doi: 10.1016/j.pain.2007.11.006. PubMed PMID: 18164820.
4: Medhurst AD, Briggs MA, Bruton G, Calver AR, Chessell I, Crook B, Davis JB, Davis RP, Foley AG, Heslop T, Hirst WD, Medhurst SJ, Ociepka S, Ray A, Regan CM, Sargent B, Schogger J, Stean TO, Trail BK, Upton N, White T, Orlek B, Wilson DM. Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats. Biochem Pharmacol. 2007 Apr 15;73(8):1182-94. PubMed PMID: 17276409.
