| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
BRL-15572 (BRL-15,572; BRL-15572; BRL 15,572; BRL15,572) dihydrochloride salt is a potent and selective 5-HT1D receptor antagonist with important biological activity. It suppresses 5-HT1D with a pKi of 7.9.
| Targets |
5-HT1D ( pKi = 7.9 ); 5-HT1A ( pKi = 7.7 ); 5-HT2B ( pKi = 7.4 ); 5-HT2A ( pKi = 6.6 ); 5-HT7 ( pKi = 6.3 )
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| ln Vitro |
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| Cell Assay |
[35S]GTPγS binding studies. Studies on the binding of [35S]GTPγS are conducted in CHO cells that express either the h5-HT1B or h5-HT1D receptors. In summary, 1 × 106 cell membranes are preincubated in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]) containing GDP (10 µ M), with or without BRL-15572, for 30 minutes at 30°C. A 100 pM assay concentration of [35S]GTPγS is added in 10 µL increments to initiate the reaction, which is then incubated for an additional 30 minutes at 30°C. The determination of non-specific binding is achieved by first adding unlabelled GTPγS (10 µM) and then adding cells. Whatman GF/B grade filters are used to quickly filter the reaction out, and five ice-cold HEPES buffer washes are then performed. Liquid scintillation spectroscopy is used to measure radioactivity.
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| Animal Protocol |
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| References |
[1]. Naunyn Schmiedebergs Arch Pharmacol . 1997 Sep;356(3):312-20. [2]. Naunyn Schmiedebergs Arch Pharmacol . 1997 Sep;356(3):321-7. [3]. Br J Pharmacol . 1999 Feb;126(3):607-12. [4]. Clin Exp Pharmacol Physiol . 2005 Oct;32(10):894-900. [5]. lin Exp Pharmacol Physiol . 2007 Nov;34(11):1199-206. [6]. Naunyn Schmiedebergs Arch Pharmacol . 2004 Jul;370(1):46-53. |
| Molecular Formula |
C25H29CL3N2O
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| Molecular Weight |
479.87
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| Exact Mass |
478.13
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| CAS # |
193611-72-2
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| Related CAS # |
BRL-15572 hydrochloride; 1173022-77-9
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| Appearance |
White to off-white solid powder
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| SMILES |
C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl
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| InChi Key |
WPEXRXMQMPOHIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27ClN2O.2ClH/c26-22-12-7-13-23(18-22)28-16-14-27(15-17-28)19-24(29)25(20-8-3-1-4-9-20)21-10-5-2-6-11-21;;/h1-13,18,24-25,29H,14-17,19H2;2*1H
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| Chemical Name |
3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol;dihydrochloride
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.33 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 (4.33 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 (4.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 20 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0839 mL | 10.4195 mL | 20.8390 mL | |
| 5 mM | 0.4168 mL | 2.0839 mL | 4.1678 mL | |
| 10 mM | 0.2084 mL | 1.0419 mL | 2.0839 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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