GR 127935 hydrochloride |
Catalog No.GC17140
One-Click Copy Product Info
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GR 127935 hydrochloride is a 5-HT1B/1D receptor antagonist that inhibits hypotensive responses.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 148642-42-6
Sample solution is provided at 25 µL, 10mM.
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GR 127935 hydrochloride is a 5-HT1B/1D receptor antagonist that inhibits hypotensive responses [1]. GR 127935 hydrochloride can irreversibly antagonize the contraction of isolated canine basilar arteries and veins induced by sumatriptan, persistently antagonize hypothermia and rotational behavior mediated by 5-HT 1D receptors in guinea pigs, and block the central 5-HT1D auto-receptors both in vitro and in vivo[2]. GR 127935 hydrochloride has been widely used to regulate the basic locomotor activity of rats and prevent excessive activity [3].
In vitro, GR 127935 hydrochloride treatment for 48 hours significantly inhibited the replication of SARS-CoV-2 virus in HEK293T-ACE2-TMPRSS2 cells, with an EC50 value of 1.6µM[4].
In vivo, GR 127935 hydrochloride treatment via a single subcutaneous injection at a dose of 3mg/kg for 1 hour significantly reversed the increase in the brain reward threshold caused by RU 24969 (1mg/kg) in rats[5]. A single intraperitoneal injection of GR 127935 hydrochloride (10mg/kg) significantly reduced the 1-hour movement distance and decreased the axillary temperature in adult male and female rats[6].
References:
[1] Sánchez-Maldonado C, López-Sánchez P, Anguiano-Robledo L, et al. GR-127935-sensitive Mechanism Mediating Hypotension in Anesthetized Rats: Are 5-HT: 5B: Receptors Involved?[J]. Journal of Cardiovascular Pharmacology, 2015, 65(4): 335-341.
[2] Skingle M, Beattie D T, Scopes D I C, et al. GR127935: a potent and selective 5-HT1D receptor antagonist[J]. Behavioural brain research, 1995, 73(1-2): 157-161.
[3] Chaouloff F, Courvoisier H, Moisan M P, et al. GR 127935 reduces basal locomotor activity and prevents RU 24969-, but not D-amphetamine-induced hyperlocomotion, in the Wistar-Kyoto hyperactive (WKHA) rat[J]. Psychopharmacology, 1999, 141(3): 326-331.
[4] Nehul S, Nagaraj S K, Narayan R, et al. A novel molecule inhibits SARS-CoV-2 RBD binding to the ACE2 receptor, blocks viral entry and exhibits antiviral activity in a murine model[J]. Archives of Virology, 2026, 171(3): 98.
[5] Harrison A A, Parsons L H, Koob G F, et al. RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist[J]. Psychopharmacology, 1999, 141(3): 242-250.
[6] McDougall S A, Roe M J, Robinson J A M, et al. Effects of the serotonin 5-HT1B receptor agonist CP 94253 on the locomotor activity and body temperature of preweanling and adult male and female rats[J]. European Journal of Pharmacology, 2022, 926: 175019.
| Cell experiment [1]: | |
Cell lines | HEK293T-ACE2-TMPRSS2 cells |
Preparation Method | HEK293T-ACE2-TMPRSS2 cells were maintained in high glucose DMEM complemented with 10% FBS, 100units of penicillin, and 100µg/ml streptomycin in a humidified incubator at 37°C and 5% CO2. The day before the pseudovirus assay, HEK-293T-hACE2-TMPRSS2 cells (0.5×106 cells per well) were seeded into a gelatin-coated 96-well plate (0.1%). The next day, two-fold serial dilutions of GR 127935 hydrochloride were prepared in 2% DMEM, producing final concentrations (0.02, 0.1, 1, 5, 10, and 15μM). The serially diluted GR 127935 hydrochloride was mixed in equal volumes with the virus (1×106 RLU/mL) supplemented with 10mg/ml hexadimethrine bromide and incubated for 30min at 37°C in a 5% CO2 incubator. Subsequently, each dilution was then added to HEK-293T cells expressing human ACE2-TMPRSS2. The plate was then incubated at 37°C in a 5% CO2 incubator for 60h, after which the cell lysate was prepared and used for the luciferase assay. |
Reaction Conditions | 0.02, 0.1, 1, 5, 10, and 15μM; 60h |
Applications | GR 127935 hydrochloride treatment significantly inhibited the entry of pseudovirus particles into HEK293T-ACE2-TMPRSS2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Sprague-Dawley rats were housed in large polycarbonate maternity cages on ventilated racks at 22-23°C and kept under a 12:12 light/dark cycle. Food and water were freely available. Behavioral testing was done in activity monitoring chambers that consisted of acrylic walls, a plastic floor, and an open top. Each chamber included an X-Y photobeam array, with 16 photocells and detectors, that was used to determine distance traveled (locomotor activity). Rats were injected intraperitoneally with saline vehicle or GR 127935 hydrochloride (10mg/kg) and immediately placed in activity chambers, where distance traveled (i.e., horizontal locomotor activity) was measured for 60min. |
Dosage form | 10mg/kg for once; i.p. |
Applications | GR 127935 hydrochloride treatment significantly reduced the 1-hour movement distance in rats. |
References: | |
| Cas No. | 148642-42-6 | SDF | |
| Chemical Name | N-(4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride | ||
| Canonical SMILES | O=C(C(C=C1)=CC=C1C2=CC=C(C3=NOC(C)=N3)C=C2C)NC4=CC=C(C(N5CCN(C)CC5)=C4)OC.Cl | ||
| Formula | C29H31N5O3.HCl | M.Wt | 534.06 |
| Solubility | DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.25 mg/ml | Storage | Store at 2-8°C |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8724 mL | 9.3622 mL | 18.7245 mL |
| 5 mM | 374.5 μL | 1.8724 mL | 3.7449 mL |
| 10 mM | 187.2 μL | 936.2 μL | 1.8724 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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 32 reference(s) in Google Scholar.)