Synonym
GR 114297A; GR114297A; GR-114297A; GR 114297X; GR114297X; GR-114297X; Picumeterol fumarate
IUPAC/Chemical Name
Benzenemethanol, 4-amino-3,5-dichloro-alpha-(((6-(2-(2-pyridinyl)ethoxy)hexyl)amino)methyl)-, (R)-, (E)-2-butenedioate (2:1) (salt);
InChi Key
MZHXOYZUNRCUCP-MMSVOLSESA-N
InChi Code
InChI=1S/2C21H29Cl2N3O2.C4H4O4/c2*22-18-13-16(14-19(23)21(18)24)20(27)15-25-9-4-1-2-6-11-28-12-8-17-7-3-5-10-26-17;5-3(6)1-2-4(7)8/h2*3,5,7,10,13-14,20,25,27H,1-2,4,6,8-9,11-12,15,24H2;1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*20-;/m00./s1
SMILES Code
Nc1c(Cl)cc(cc1Cl)[C@@H](O)CNCCCCCCOCCc2ccccn2.Nc3c(Cl)cc(cc3Cl)[C@@H](O)CNCCCCCCOCCc4ccccn4.OC(=O)\C=C\C(=O)O
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
968.84
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: Weersink EJ, Postma DS, Koëter GH, Man Y, Nials AT, Coleman RA. Picumeterol: dissociation of improvement in lung function and reduction of airways hyperresponsiveness in asthmatics. Br J Clin Pharmacol. 1997 Feb;43(2):169-76. PubMed PMID: 9131949; PubMed Central PMCID: PMC2042730.
2: Barrow A, Camp SJ, Dayal S, Jenner WN, Lashmar D, Oxford JM, Palmer E, Scully NL, Curtis GC, Hughes HM, et al. Kinetics and disposition of picumeterol in animals. Xenobiotica. 1995 Sep;25(9):993-1007. PubMed PMID: 8553692.
3: Waldeck B. Some pharmacodynamic aspects on long-acting beta-adrenoceptor agonists. Gen Pharmacol. 1996 Jun;27(4):575-80. Review. PubMed PMID: 8853286.
4: Yan D, Hamed O, Joshi T, Mostafa MM, Jamieson KC, Joshi R, Newton R, Giembycz MA. Analysis of the Indacaterol-Regulated Transcriptome in Human Airway Epithelial Cells Implicates Gene Expression Changes in the Adverse and Therapeutic Effects of β(2)-Adrenoceptor Agonists. J Pharmacol Exp Ther. 2018 Jul;366(1):220-236. doi: 10.1124/jpet.118.249292. Epub 2018 Apr 13. PubMed PMID: 29653961.
