GLPBio

GR 127935 hydrochloride

Catalog No.: GC17140Purity:>98.00%
COASDSData Sheet
GR 127935 hydrochloride is a 5-HT1B/1D receptor antagonist that inhibits hypotensive responses.

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GR 127935 hydrochloride
Cas No.: 148642-42-6
1mgIn Stock
$35.00
1
5mgIn Stock
$106.00
1
10mgIn Stock
$192.00
1
25mgIn Stock
$399.00
1
50mgIn Stock
$745.00
1
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Description

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.

Protocol

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:
[1] 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.
[2] 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
148642-42-6
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
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
Molecular Formula
C29H31N5O3.HCl
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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