GR 46611 |
Catalog No.GC14373
One-Click Copy Product Info
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GR 46611 is a 5-HT1B and 5-HT1D receptor agonist, which can regulate the feeding behavior of animals.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 185259-85-2
Sample solution is provided at 25 µL, 10mM.
GR 46611 is a 5-HT1B and 5-HT1D receptor agonist, which can regulate the feeding behavior of animals[1]. GR 46611 enhances transporter ZnT8-dependent zinc import into insulin granules through stimulation of V-ATPase-driven acidification in β-cells and increases β-cell zinc content and augments β-cell-targeted drug delivery [2]. GR 46611 has been widely used in rat formalin tests to alleviate inflammatory pain [3].
In vitro, GR 46611 treatment (1μM) for 48 hours significantly promoted the proliferation of CCRF-CEM cells[4].
In vivo, GR 46611 treatment via daily intraperitoneal injection at a dose of 1mg/kg for 14 days significantly increased the seizure threshold of Dravet syndrome (DS) mice induced by hyperthermia, and reduced the severity of seizures and increased the survival rate of the mice[5]. A single injection of GR 46611 (30mg/kg) was administered, lasting for 3 hours, which significantly caused a decrease in rectal temperature in adult guinea pigs[6]. A single injection of GR 46611 (0.6nM; 1µl) via anterior portion of paraventricular thalamic nucleus reduced the pain threshold of mice within 24 hours and prolonged the immobility time in the forced swimming test (FST) and tail suspension test (TST)[7].
References:
[1] Da Silva R A, de Oliveira S T, Hackl L P N, et al. Ingestive behaviors and metabolic fuels after central injections of 5-HT1A and 5-HT1D/1B receptors agonists in the pigeon[J]. Brain research, 2004, 1026(2): 275-283.
[2] Lee S, Fraser H P, Schugar R C, et al. Pharmacologic stimulation of insulin granule acidification increases β-cell zinc content and augments β-cell-targeted drug delivery[J]. Journal of Biological Chemistry, 2025, 301(10).
[3] Granados-Soto V, Argüelles C F, Rocha-González H I, et al. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats[J]. Neuroscience, 2010, 165(2): 561-568.
[4] Sibella-Argüelles C. The proliferation of human T lymphoblastic cells induced by 5-HT1B receptors activation is regulated by 5-HT-moduline[J]. Comptes Rendus de l'Académie des Sciences-Series III-Sciences de la Vie, 2001, 324(4): 365-372.
[5] Hatini P G, Commons K G. A 5‐HT1D‐receptor agonist protects Dravet syndrome mice from seizure and early death[J]. European Journal of Neuroscience, 2020, 52(10): 4370-4374.
[6] Skingle M, Higgins G A, Feniuk W. Stimulation of central 5-HT1D receptors causes hypothermia in the guinea-pig[J]. Journal of Psychopharmacology, 1994, 8(1): 14-21.
[7] Cui M, Ji R, Song L, et al. Neuronal and molecular mechanisms underlying chronic pain and depression comorbidity in the paraventricular thalamus[J]. Journal of Neuroscience, 2024, 44(13).
| Cell experiment [1]: | |
Cell lines | CCRF CEM cells |
Preparation Method | CCRF CEM cells were cultured in RPMI-1640 medium supplemented with 10% heat-inactivated fetal bovine serum, 100U/ml penicillin, 100μg/ml streptomycin in a humidified incubator at 37°C and 5% CO2. CCRF CEM cells were plated at a density of 2×105 cells/well in a 6-well plate with growth medium for 24h, and then were incubated with 1μM GR 46611 for 48h, the cell proliferation was analyzed. |
Reaction Conditions | 1μM; 48h |
Applications | GR 46611 treatment significantly enhanced cell proliferation of CCRF CEM cells. |
| Animal experiment [2]: | |
Animal models | Dravet syndrome (DS) mice |
Preparation Method | DS mice were primed with a hyperthermia-induced seizure on postnatal day of age (P) 18±1 day. After a 5-min acclimation to a RET-3 rectal temperature probe, body temperature was raised at a rate of 0.25°C per minute using a heat lamp until the first generalized seizure resulting in a loss of posture. Subsequently, the same mice were tested for seizure threshold at P21 after receiving drug pretreatment (GR 46611 was dissolved in 5% DMSO, 30% propylene glycol in saline and administered intraperitoneally at 1mg/kg) 20min before repeating the hyperthermia protocol. |
Dosage form | 1mg/kg for once; i.p. |
Applications | GR 46611 treatment increased the threshold of hyperthermia-induced seizure and lowered seizure severity in DS mice. |
References: | |
| Cas No. | 185259-85-2 | SDF | |
| Chemical Name | (Z)-3-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)-N-(4-methoxybenzyl)acrylamide | ||
| Canonical SMILES | O=C(/C=C\C1=CC=C2NC=C(C2=C1)CCN(C)C)NCC(C=C3)=CC=C3OC | ||
| Formula | C23H27N3O2 | M.Wt | 377.49 |
| Solubility | Soluble to 50 mM in DMSO and to 10 mM in ethanol | Storage | Store at RT |
| 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 | 2.6491 mL | 13.2454 mL | 26.4908 mL |
| 5 mM | 529.8 μL | 2.6491 mL | 5.2982 mL |
| 10 mM | 264.9 μL | 1.3245 mL | 2.6491 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)