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RS 79948 hydrochloride

CAS# 186002-54-0

RS 79948 hydrochloride

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Chemical structure

RS 79948 hydrochloride

3D structure

Chemical Properties of RS 79948 hydrochloride

Cas No. 186002-54-0 SDF Download SDF
PubChem ID 9908991 Appearance Powder
Formula C19H29ClN2O3S M.Wt 400.96
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 25 mM in water
Chemical Name (8aR,12aS,13aS)-12-ethylsulfonyl-3-methoxy-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine;hydrochloride
SMILES CCS(=O)(=O)N1CCCC2C1CC3C4=C(CCN3C2)C=C(C=C4)OC.Cl
Standard InChIKey DZTZUOBWDBPPJQ-BQBHMPFISA-N
Standard InChI InChI=1S/C19H28N2O3S.ClH/c1-3-25(22,23)21-9-4-5-15-13-20-10-8-14-11-16(24-2)6-7-17(14)19(20)12-18(15)21;/h6-7,11,15,18-19H,3-5,8-10,12-13H2,1-2H3;1H/t15-,18+,19+;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of RS 79948 hydrochloride

Descriptionα2-adrenoreceptor antagonist (Kd values are; 0.18, 0.19 and 0.42 nM for α2B α2C and α2A, respectively in rat).

RS 79948 hydrochloride Dilution Calculator

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RS 79948 hydrochloride Molarity Calculator

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Preparing Stock Solutions of RS 79948 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.494 mL 12.4701 mL 24.9401 mL 49.8803 mL 62.3504 mL
5 mM 0.4988 mL 2.494 mL 4.988 mL 9.9761 mL 12.4701 mL
10 mM 0.2494 mL 1.247 mL 2.494 mL 4.988 mL 6.235 mL
50 mM 0.0499 mL 0.2494 mL 0.4988 mL 0.9976 mL 1.247 mL
100 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.4988 mL 0.6235 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on RS 79948 hydrochloride

[3H]RS79948-197 binding to human, rat, guinea pig and pig alpha2A-, alpha2B- and alpha2C-adrenoceptors. Comparison with MK912, RX821002, rauwolscine and yohimbine.[Pubmed:9551719]

Eur J Pharmacol. 1998 Feb 5;343(1):93-101.

The Kd values of the recently introduced radioligand [3H]RS79948-197 ((8a R,12aS,13a-S)-5,8,8a,9,10,11,12,12a,13,13a-decahydro-3-metho xy-12-(ethylsulphonyl)-6H-isoquino[2,1-g][1,6]naphthyridine) were determined for the recombinant human and rat alpha2A-, alpha2B- and alpha2C- as well as guinea pig alpha2B- and alpha2c-adrenoceptors expressed in COS (CV-1 Origin, SV40) cells. In addition, the Kd values were also determined for [3H]RS79948-197 for the guinea pig spleen alpha2A-adrenoceptor and for pig alpha2A-, alpha2B- and alpha2C-adrenoceptors in membranes obtained from kidney and striatum. Available radioligands for alpha2-adrenoceptors, besides [3H]RS79948-197 are the tritiated forms of MK912 ((2S,12bS)1',3'-dimethylspiro(1,3,4,5',6,6',7,12b-octa hydro-2H-benzo[b]furo[2,3-a]quinazoline)-2,4'-pyrimidin-2'-one), RX821002 (2-methoxy-idazoxan), rauwolscine and yohimbine. In the present article the binding constants of all these substances for the alpha2A-, alpha2B- and alpha2C-adrenoceptor subtypes in human, pig, rat and guinea pig are reviewed. In all species tested MK912 was alpha2C-selective, RX821002 showed a minor alpha2A-selectivity, whereas [3H]RS79948-197 was non-selective among the alpha2-adrenoceptor subtypes, showing high affinity for all three subtypes. Rauwolscine and yohimbine showed relatively low affinities for nmost of the alpha2-adrenoceptor subtypes investigated, the exception being rauwolscine having high affinity for the human and porcine alpha2C-adrenoceptors.

Evaluation in rat of RS-79948-197 as a potential PET ligand for central alpha 2-adrenoceptors.[Pubmed:8982721]

Eur J Pharmacol. 1996 Dec 12;317(1):67-73.

Tritium-labelled RS-79948-197 {(8aR,12aS,13aS)-5, 8,8a,9,10,11,12,12a,13,13a-decahydro-3-methoxy-12-(ethylsulphon yl)-6H-iso- quino[2,1-g][1,6]naphthyridine} was evaluated in rat brain as an in vivo ligand for central alpha 2-adrenoceptors, as a preliminary step in the development of a radioligand for positron-emission tomography (PET) studies. The maximal receptor-specific signal was achieved within 90-120 min after i.v. injection of [ethyl-3H]RS-79948-197 and was selective for the alpha 2- compared with the alpha 1-adrenoceptor, with no detectable binding to the imidazoline-I2 site. Estimates for binding potential (approximating to Bmax/Kd) ranged between 3.4 in entorhinal cortex and 0.5 in medulla oblongata. The results, which indicate a similarly localised but 2-fold increase in specific binding compared with that previously demonstrated using [3H]RX 821002 (2-methoxy-idazoxan), are sufficiently encouraging as to support further investment in the development of 11C-labelled RS-79948-197, or a close structural analogue, as a ligand for clinical PET.

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