| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
The primary molecular targets of GR-55562 dihydrobromide are the 5-HT1B and 5-HT1D serotonin receptors, which are G protein-coupled receptors that inhibit adenylate cyclase and modulate neurotransmitter release. GR-55562 acts as a selective antagonist, blocking 5-HT1B/5-HT1D receptor-mediated signaling. These receptors are involved in the regulation of cranial vasoconstriction and neurogenic inflammation, making them relevant to migraine pathophysiology.
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| ln Vitro |
In vitro, GR-55562 dihydrobromide is a selective 5-HT1B/5-HT1D serotonin receptor antagonist with high affinity for these subtypes. It blocks 5-HT1B/5-HT1D receptor-mediated signaling in radioligand binding assays and functional assays. GR-55562 demonstrates selectivity over other 5-HT receptor subtypes, making it a valuable tool for studying serotonin receptor pharmacology.
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| ln Vivo |
No dedicated in vivo efficacy studies have been published specifically for GR-55562 dihydrobromide. As a research tool for 5-HT1B/5-HT1D receptor pharmacology, its in vivo applications are primarily in preclinical models of migraine, anxiety, and other neurological diseases. No pharmacokinetic parameters, maximum tolerated doses, or in vivo efficacy data are available in the published literature.
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| Enzyme Assay |
Non-cell-based assays for GR-55562 dihydrobromide use radioligand binding with [3H]5-HT or [125I]iodocyanopindolol in membrane preparations from cells expressing recombinant 5-HT1B or 5-HT1D receptors or guinea pig brain cortex. Membranes are incubated with radioligand and increasing concentrations of GR-55562 in assay buffer. Bound radioligand is separated by rapid filtration, and radioactivity is quantified.
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| Cell Assay |
Cell-based assays for GR-55562 dihydrobromide use 5-HT1B/5-HT1D receptor-expressing cell lines such as CHO-K1 or HEK293 cells. Cells are cultured in standard medium, and 5-HT1B/5-HT1D receptor-mediated signaling is measured by cAMP inhibition assay or [35S]GTPγS binding. GR-55562 is added at varying concentrations to determine antagonist potency.
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| Animal Protocol |
No specific in vivo animal protocols have been established for GR-55562 dihydrobromide. For potential evaluation, the compound could be administered intraperitoneally or subcutaneously in rodent models of migraine or anxiety. Doses would be determined from pharmacokinetic studies. Endpoints could include neurogenic inflammation, cranial vasoconstriction, and behavioral measures of anxiety. No validated therapeutic protocols exist for this research compound.
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| References | |
| Additional Infomation |
3-[3-(dimethylamino)propyl]-4-hydroxy-N-(4-pyridin-4-ylphenyl)benzamide is a member of the benzamide class of compounds.
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| Molecular Formula |
C23H27BR2N3O2
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|---|---|
| Molecular Weight |
411.92444
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| Exact Mass |
447.148
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| CAS # |
172854-55-6
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| Related CAS # |
GR 55562 dihydrochloride;159533-25-2
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| PubChem CID |
128018
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.192g/cm3
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| Boiling Point |
511.6ºC at 760 mmHg
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| Flash Point |
263.2ºC
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| Vapour Pressure |
4.36E-11mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
5.877
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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 |
7
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| Heavy Atom Count |
28
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.CN(C)CCCC1=C(O)C=CC(C(NC2C=CC(C3C=CN=CC=3)=CC=2)=O)=C1
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| InChi Key |
RDAZGSSTKFYEKH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N3O2.2BrH/c1-26(2)15-3-4-19-16-20(7-10-22(19)27)23(28)25-21-8-5-17(6-9-21)18-11-13-24-14-12-18/h5-14,16,27H,3-4,15H2,1-2H3,(H,25,28)2*1H
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| Chemical Name |
3-[3-(Dimethylamino)propyl]-4-hydroxy-N-[4-(4-pyridinyl)phenyl]benzamide dihydrobromide
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| Synonyms |
GR-55562 dihydrobromide GR55562 dihydrobromide GR 55562 dihydrobromide
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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 |
| 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) |
H2O: ≥ 25 mg/mL (~60.7 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4277 mL | 12.1383 mL | 24.2766 mL | |
| 5 mM | 0.4855 mL | 2.4277 mL | 4.8553 mL | |
| 10 mM | 0.2428 mL | 1.2138 mL | 2.4277 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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