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MedKoo Cat#: 414283 | Name: L 657743

Description:

WARNING: This product is for research use only, not for human or veterinary use.

L 657743 is an Adrenergic alpha-Antagonist.

Chemical Structure

L 657743
L 657743
CAS#111466-41-2

Theoretical Analysis

MedKoo Cat#: 414283

Name: L 657743

CAS#: 111466-41-2

Chemical Formula: C20H25N3O2

Exact Mass: 339.1947

Molecular Weight: 339.44

Elemental Analysis: C, 70.77; H, 7.42; N, 12.38; O, 9.43

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Related CAS #
No Data
Synonym
L657743; L-657743; L 657743; MK912; MK-912; MK 912; M7065; M-7065; M 7065
IUPAC/Chemical Name
Spiro(2H-benzofuro(2,3-a)quinolizine-2,4'(1'H)-pyrimidin)-2'(3'H)-one, 1,3,4,5',6,6',7,12b-octahydro-1',3'-dimethyl-, (2S-trans)-
InChi Key
JRDUBBHIPPPSLP-OXJNMPFZSA-N
InChi Code
InChI=1S/C20H25N3O2/c1-21-11-8-20(22(2)19(21)24)9-12-23-10-7-15-14-5-3-4-6-17(14)25-18(15)16(23)13-20/h3-6,16H,7-13H2,1-2H3/t16-,20+/m0/s1
SMILES Code
O=C1N(C)[C@]2(CCN1C)CCN3CCC4=C(OC5=CC=CC=C54)[C@]3([H])C2
Appearance
Solid powder
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
L 657743 is an Adrenergic alpha-Antagonist.
In vitro activity:
TBD
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 339.44 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.

Recalculate based on batch purity %
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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Clineschmidt BV, Pettibone DJ, Lotti VJ, Hucker HB, Sweeney BM, Reiss DR, Lis EV, Huff JR, Vacca J. A peripherally acting alpha-2 adrenoceptor antagonist: L-659,066. J Pharmacol Exp Ther. 1988 Apr;245(1):32-40. PMID: 2896239. 2: Campbell WR, Potter DE. The central effects of moxonidine on intraocular pressure and its antagonism by L-659, 066 and L-657, 743 in the rabbit. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Oct;18(6):1051-61. doi: 10.1016/0278-5846(94)90130-9. PMID: 7824759. 3: Jantschak F, Pertz HH. Alpha2C-adrenoceptors play a prominent role in sympathetic constriction of porcine pulmonary arteries. Naunyn Schmiedebergs Arch Pharmacol. 2012 Jun;385(6):595-603. doi: 10.1007/s00210-012-0741-3. Epub 2012 Feb 28. PMID: 22371269. 4: Jantschak F, Popp AM, Hofmann RA, Villalón CM, Centurión D, Pertz HH. Postjunctional α2C-adrenoceptors mediate vasoconstriction in rat tail artery: influence of precontraction and temperature on vasoreactivity. Naunyn Schmiedebergs Arch Pharmacol. 2010 Dec;382(5-6):487-97. doi: 10.1007/s00210-010-0564-z. Epub 2010 Sep 24. PMID: 20862454. 5: Kawamura K, Akiyama M, Yui J, Yamasaki T, Hatori A, Kumata K, Wakizaka H, Takei M, Nengaki N, Yanamoto K, Fukumura T, Zhang MR. In vivo evaluation of limiting brain penetration of probes for α(2C)-adrenoceptor using small-animal positron emission tomography. ACS Chem Neurosci. 2010 Jul 21;1(7):520-8. doi: 10.1021/cn1000364. Epub 2010 Jun 2. PMID: 22778842; PMCID: PMC3368684. 6: Robichaud A, Savoie C, Stamatiou PB, Lachance N, Jolicoeur P, Rasori R, Chan CC. Assessing the emetic potential of PDE4 inhibitors in rats. Br J Pharmacol. 2002 Jan;135(1):113-8. doi: 10.1038/sj.bjp.0704457. PMID: 11786486; PMCID: PMC1573119. 7: Murrin LC, Gerety ME, Happe HK, Bylund DB. Inverse agonism at alpha(2)-adrenoceptors in native tissue. Eur J Pharmacol. 2000 Jun 16;398(2):185-91. doi: 10.1016/s0014-2999(00)00317-4. PMID: 10854829. 8: Näreoja K, Näsman J. Characterization of α(2B)-adrenoceptor ligand binding in the presence of muscarinic toxin α and delineation of structural features of receptor binding selectivity. Eur J Pharmacol. 2012 May 15;683(1-3):63-70. doi: 10.1016/j.ejphar.2012.03.028. Epub 2012 Mar 23. PMID: 22465183. 9: Kashihara T, Goto K, Sahara Y, Nakayama K, Ishikawa T. Differential involvement of alpha1-adrenoceptors in vasoconstrictor responses to cooling in mouse plantar arteries in vitro and in vivo. J Smooth Muscle Res. 2009 Jun;45(2-3):87-95. doi: 10.1540/jsmr.45.87. PMID: 19602853. 10: Trendelenburg AU, Wahl CA, Starke K. Antagonists that differentiate between alpha 2A-and alpha 2D-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1996 Feb;353(3):245-9. doi: 10.1007/BF00168625. PMID: 8692278.