GR127935
Based on 1 Customer Validation
GR127935 is a selective and orally active 5-HT1D and 5-HT1B receptor antagonist with pKi values of 8.5 for both receptors. GR127935 impairs memory acquisition and Serotonin (HY-B1473A)-mediated vasodilation. GR127935 can be used for research on amnesia, neuroendocrine cancer, and migraine.
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 148672-13-3
- Formula: C29H31N5O3
- Molecular Weight:497.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[3]|
5-HT1A Receptor 6.5 (pKi) |
5-HT1B Receptor 8.5 (pKi) |
5-HT1D Receptor 8.5 (pKi) |
5-HT2A Receptor 6.4 (pKi) |
In Vitro
GR127935 (0.1 μM; 30 min) impairs serotonin-mediated vasodilation in isolated mesenteric arteries from VEH J:Nu nude mice, but does not impair vasodilation from BON-1 NET tumor-bearing mice[2].
GR127935 is a potent and selective 5-HT1D receptor antagonist with a pKi of 8.5 at guinea pig striatal 5-HT1D receptors, exhibiting 100-fold selectivity over 5-HT1A and 5-HT2C receptors[3].
GR127935 (1-10 nM) effectively antagonizes Sumatriptan (HY-B0121B)-induced contraction of isolated canine saphenous vein at 1 and 10 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GR127935 (0.005-0.5 ng/mouse; intra-CA1) exerts an amnesic effect on memory acquisition at 0.05 and 0.5 ng/mouse, whereas 0.005 ng/mouse is subthreshold, without affecting locomotor activity or tail flick in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI mice (male, 25-30 g, 5-8 weeks old)[1]
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Dosage:0.005 ng/mouse
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Administration:intra-CA1; single injection; 5 min before training
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Result:Reversed impairment of memory acquisition induced by harmaline (1 mg/kg, i.p.).
Did not alter locomotor activity or tail flick behaviors.
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Animal Model:NMRI mice (male, 25-30 g, 5-8 weeks old)[1]
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Dosage:0.005-0.5 ng/mouse
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Administration:intra-CA1; single injection; 5 min before training
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Result:Impaired memory acquisition at 0.05 and 0.5 ng/mouse (decreased step-down latency).
Did not impair memory acquisition at 0.005 ng/mouse.
Did not alter locomotor activity or tail flick behavior.
Chemical Information
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CAS No. 148672-13-3
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Appearance Solid
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Molecular Weight 497.59
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Formula C29H31N5O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OC)C(N2CCN(C)CC2)=C1)C3=CC=C(C4=CC=C(C5=NOC(C)=N5)C=C4C)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (200.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Nasehi M, et al. Possible involvement of CA1 5-HT1B/1D and 5-HT2A/2B/2C receptors in harmaline-induced amnesia. Pharmacol Biochem Behav. 2014 Oct;125:70-77. [Content Brief]
[3]. J W Clitherow, et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists. J Med Chem. 1994 Jul 22;37(15):2253-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0097 mL | 10.0484 mL | 20.0969 mL | 50.2422 mL |
| 5 mM | 0.4019 mL | 2.0097 mL | 4.0194 mL | 10.0484 mL | |
| 10 mM | 0.2010 mL | 1.0048 mL | 2.0097 mL | 5.0242 mL | |
| 15 mM | 0.1340 mL | 0.6699 mL | 1.3398 mL | 3.3495 mL | |
| 20 mM | 0.1005 mL | 0.5024 mL | 1.0048 mL | 2.5121 mL | |
| 25 mM | 0.0804 mL | 0.4019 mL | 0.8039 mL | 2.0097 mL | |
| 30 mM | 0.0670 mL | 0.3349 mL | 0.6699 mL | 1.6747 mL | |
| 40 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2561 mL | |
| 50 mM | 0.0402 mL | 0.2010 mL | 0.4019 mL | 1.0048 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3349 mL | 0.8374 mL | |
| 80 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6280 mL | |
| 100 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5024 mL |
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