SB 277011A dihydrochloride (Synonyms: SB-277011A dihydrochloride) |
Katalog-Nr.GC13183
One-Click Copy Product Info
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SB 277011A-Dihydrochlorid (SB-277011A-Dihydrochlorid) ist ein potenter, selektiver, oral bioverfÜgbarer und in das Gehirn eindringender Dopamin-D3-Rezeptorantagonist mit pKis-Werten von 8,0, 6,0, < 5,2 und 5,9 fÜr D3-, D2-, 5-HT1B- und 5-HT1D-Rezeptoren , beziehungsweise.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1226917-67-4
Sample solution is provided at 25 µL, 10mM.
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SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1].
SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].
References:
[1]. Stemp G, et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4;43(9):1878-85.
| Cas No. | 1226917-67-4 | SDF | |
| Überlieferungen | SB-277011A dihydrochloride | ||
| Chemical Name | N-((1r,4r)-4-(2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)quinoline-4-carboxamide dihydrochloride | ||
| Canonical SMILES | N#CC1=CC(CCN2CC[C@@]3([H])CC[C@@](NC(C4=CC=NC5=CC=CC=C45)=O)([H])CC3)=C(C2)C=C1.Cl.Cl | ||
| Formula | C28H30N4O.2HCl | M.Wt | 511.49 |
| Löslichkeit | DMF: 3 mg/ml,DMSO: 14 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml,Ethanol: 0.1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9551 mL | 9.7754 mL | 19.5507 mL |
| 5 mM | 391 μL | 1.9551 mL | 3.9101 mL |
| 10 mM | 195.5 μL | 977.5 μL | 1.9551 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)