Synonym
Tibalosin; CP804S; CP-804S; CP 804S
IUPAC/Chemical Name
Benzo(b)thiophene-5-methanol, 2,3-dihydro-alpha-(1-((4-phenylbutyl)amino)ethyl)-, (R*,S*)-(+-)-
InChi Key
FJLRGFADCXTJNV-KKSFZXQISA-N
InChi Code
InChI=1S/C21H27NOS/c1-16(22-13-6-5-9-17-7-3-2-4-8-17)21(23)19-10-11-20-18(15-19)12-14-24-20/h2-4,7-8,10-11,15-16,21-23H,5-6,9,12-14H2,1H3/t16-,21-/m0/s1
SMILES Code
O[C@@H]([C@@H](NCCCCC1=CC=CC=C1)C)C2=CC=C3C(CCS3)=C2
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
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| Soluble in DMSO |
0.0 |
100.00 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
341.51
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: Qian JQ, Mathy MJ, Thoolen MJ, Timmermans PB, van Zwieten PA. Antihypertensive activity and interaction with alpha-adrenoceptors of tibalosine ([1-(2, 3-dihydro-5-benzo-(b)-thienyl)-2-(4-phenyl-butylamino)-1-propanol], CP 804 S) in rat and cat preparations. Arch Int Pharmacodyn Ther. 1983 Dec;266(2):264-81. PMID: 6141776.
2: Chatelain P, Claeys M, van Dorsser W, Roba J. Antihypertensive activity of tibalosine (CP 804 S) in the rat. Possible involvement of a central alpha 1-adrenergic receptor blockade. Arch Int Pharmacodyn Ther. 1984 Apr;268(2):271-86. PMID: 6145397.
3: Staessen J, Fagard R, Fiocchi R, Lijnen P, M'Buyamba-Kabangu JR, Amery A. Chronic treatment with tibalosine in essential hypertension. Arch Int Pharmacodyn Ther. 1986 Jan;279(1):162-76. PMID: 3516092.
4: Staessen J, Fagard R, Grauwels R, Lijnen P, Verschueren LJ, Amery A. Effects of tibalosine, a new alpha-adrenoceptor antagonist, in essential hypertension. Clin Pharmacol Ther. 1983 May;33(5):556-64. doi: 10.1038/clpt.1983.76. PMID: 6132697.
5: Beart PM, Schousboe A, Frandsen A. Blockade by polyamine NMDA antagonists related to ifenprodil of NMDA-induced synthesis of cyclic GMP, increases in calcium and cytotoxicity in cultured neurones. Br J Pharmacol. 1995 Apr;114(7):1359-64. doi: 10.1111/j.1476-5381.1995.tb13356.x. PMID: 7606339; PMCID: PMC1510270.
6: Staessen J, Fiocchi R, Fagard R, Lijnen P, Amery A. Alpha-adrenoceptor blockade by tibalosine: hemodynamic and humoral effects at rest and during exercise, and effect of opioid receptor antagonism. J Cardiovasc Pharmacol. 1986 Sep-Oct;8(5):1028-34. PMID: 2429076.
7: Chatelain P, Friedhoff AJ, Meller E, Mennini T, Gorissen H, Roba J. Receptor binding profile of tibalosine, a new antihypertensive. Arzneimittelforschung. 1984;34(7):754-8. PMID: 6093823.
8: Lijnen P, Staessen J, Fagard R, Amery A. Influence of central alpha 1 inhibition in patients with essential hypertension. Chest. 1983 Feb;83(2 Suppl):371-3. doi: 10.1378/chest.83.2.371. PMID: 6129952.
9: Beart PM, Ryan MC, Mercer LD, Jarrott B, Wong MG. Heterocyclic amino alcohols related to ifenprodil as sigma receptor ligands: binding and conformational analyses. Eur J Pharmacol. 1994 Oct 14;269(2):193-200. doi: 10.1016/0922-4106(94)90086-8. PMID: 7851495.
