| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
D3 Receptor 10.7-11.2 nM (Ki) D2 Receptor 5-HT1D Receptor 5-HT1B Receptor
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|---|---|
| ln Vivo |
The rat SB-277011 hydrochloride has a clean P450 profile, a brain:blood ratio of 3.6:1, an oral bioavailability of 43%, a half-life of 2.0 hours, and a plasma clearance of 19 milliliters per minute/kg. It also has an outstanding pharmacokinetic profile[1]. In rats, quinelorane at 93 mg/kg in the striatum is not reversed by SB-277011 hydrochloride (SB 277011; 3 mg/kg, po), but it is entirely reversed in the nucleus accumbens[1]. In rats, intravenous cocaine self-administration is considerably and dose-dependently reduced by SB-277011 (intraperitoneal injection; 12.5–25 mg/kg) in both low fixed-ratio and progressive-ratio reinforcement scenarios. SB-277011 can considerably reduce both basal and cocaine-enhanced rat locomotion when administered at a dose of 50 mg/kg[2].
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| References |
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| Molecular Formula |
C28H30N4O
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|---|---|
| Molecular Weight |
438.564
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| Exact Mass |
474.218
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| CAS # |
215804-67-4
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| Related CAS # |
SB-277011;215803-78-4;SB-277011 dihydrochloride;1226917-67-4
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| PubChem CID |
24845776
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
708
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45.Cl
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| InChi Key |
DKPTUMKZXQOJCX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30N4O.ClH/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27;/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33);1H
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| Chemical Name |
N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (105.26 mM)
H2O: 16.67 mg/mL (35.09 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2802 mL | 11.4009 mL | 22.8019 mL | |
| 5 mM | 0.4560 mL | 2.2802 mL | 4.5604 mL | |
| 10 mM | 0.2280 mL | 1.1401 mL | 2.2802 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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