GR127935
Based on 1 Customer Validation
GR127935 is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 can be used in neurological disease research.
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
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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
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1B Receptor 8.5 (pKi) |
5-HT1D Receptor 8.5 (pKi) |
5-HT1A Receptor 6.5 (pKi) |
5-HT2A Receptor 6.4 (pkB) |
GR127935 (1-10 nM) potently antagonizes Sumatriptan (HY-B0121B)-induced contractions in dog isolated basilar artery[1].
GR127935 (1-300 nM) blocks prejunctional 5-HT1 receptors on sympathetic nerve terminals in dog saphenous vein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GR127935 (0.005-0.5 ng/mouse, intra-CA1, 5 min before training) impairs memory acquisition in adult male NMRI mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GR56764 (1 μg in 2 μl) was unilaterally injected into the substantia nigra to induce contralateral rotations in 6-week-old guinea-pigs[1]
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Dosage:10, 30, 100, 300 μg/kg
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Administration:p.o., once
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Result:Inhibited GR56764-induced contralateral rotations in guinea-pigs, with ID50 of 28 μg/kg.
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Animal Model:Adult male NMRI mice (25-30 g, 5-8 weeks old)[2]
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Dosage:0.005, 0.05, 0.5 ng/mouse
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Administration:intra-CA1, 5 min before training
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Result:Impaired memory acquisition as shown by decreased step-down latency in the one-trial step-down passive avoidance task.
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
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)
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.
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 (272 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Skingle M, et al. GR127935: a potent and selective 5-HT1D receptor antagonist. Behav Brain Res. 1996;73(1-2):157-61. [Content Brief]
[2]. Mohammad Nasehi, 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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