Related CAS #
155418-06-7 (besilate); 155418-05-6 (free base)
Synonym
Nolpitantium besilate; SR140333B; SR-140333B; SR 140333B
IUPAC/Chemical Name
1-(2-((S)-3-(3,4-Dichlorophenyl)-1-((m-isopropoxyphenyl)acetyl)-3-piperidyl)ethyl)-4-phenylquinuclidinium benzenesulfonate
InChi Key
PQRLQZNKDQQMBC-LSYPWIJNSA-M
InChi Code
InChI=1S/C37H45Cl2N2O2.C6H6O3S/c1-28(2)43-32-11-6-8-29(24-32)25-35(42)40-19-7-14-37(27-40,31-12-13-33(38)34(39)26-31)18-23-41-20-15-36(16-21-41,17-22-41)30-9-4-3-5-10-30;7-10(8,9)6-4-2-1-3-5-6/h3-6,8-13,24,26,28H,7,14-23,25,27H2,1-2H3;1-5H,(H,7,8,9)/q+1;/p-1/t36?,37-,41?;/m1./s1
SMILES Code
O=C(N1C[C@@](CC[N+]23CCC(CC3)(C4=CC=CC=C4)CC2)(C5=CC=C(Cl)C(Cl)=C5)CCC1)CC6=CC=CC(OC(C)C)=C6.O=S(C7=CC=CC=C7)([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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
777.84
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 |
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3: Moreaux B, Nemmar A, Vincke G, Halloy D, Beerens D, Advenier C, Gustin P. Role of substance P and tachykinin receptor antagonists in citric acid-induced cough in pigs. Eur J Pharmacol. 2000 Nov 24;408(3):305-12. doi: 10.1016/s0014-2999(00)00763-9. PMID: 11090648.
4: Umer A, Ługowska-Umer H, Schönborn-Kellenberger O, Korolkiewicz PK, Sein- Anand Ł, Kocic I, Korolkiewicz RP. Tachykinin antagonists ameliorate surgically induced impairment of gastrointestinal motility in rats. Fundam Clin Pharmacol. 2020 Oct 15. doi: 10.1111/fcp.12616. Epub ahead of print. PMID: 33058252.
5: Abey HT, Fairlie DP, Moffatt JD, Balzary RW, Cocks TM. Protease-activated receptor-2 peptides activate neurokinin-1 receptors in the mouse isolated trachea. J Pharmacol Exp Ther. 2006 May;317(2):598-605. doi: 10.1124/jpet.105.097121. Epub 2006 Jan 24. PMID: 16434565.
6: Seegers HC, Hood VC, Kidd BL, Cruwys SC, Walsh DA. Enhancement of angiogenesis by endogenous substance P release and neurokinin-1 receptors during neurogenic inflammation. J Pharmacol Exp Ther. 2003 Jul;306(1):8-12. doi: 10.1124/jpet.103.050013. Epub 2003 Mar 26. PMID: 12660314.
7: Boichot E, Germain N, Emonds-Alt X, Advenier C, Lagente V. Effects of SR 140333 and SR 48968 on antigen and substance P-induced activation of guinea-pig alveolar macrophages. Clin Exp Allergy. 1998 Oct;28(10):1299-305. doi: 10.1046/j.1365-2222.1998.00398.x. PMID: 9824398.
8: Daoui S, Cui YY, Lagente V, Emonds-Alt X, Advenier C. A tachykinin NK3 receptor antagonist, SR 142801 (osanetant), prevents substance P-induced bronchial hyperreactivity in guinea-pigs. Pulm Pharmacol Ther. 1997 Oct- Dec;10(5-6):261-70. doi: 10.1006/pupt.1998.0104. PMID: 9778489.
