2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. GR127935

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.

GR127935

GR127935 Chemical Structure

CAS No. : 148672-13-3

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GR127935:

GR127935 Related Antibodies

Top Publications Citing Use of Products

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[3]

5-HT1B Receptor

8.5 (pKi)

5-HT1D Receptor

8.5 (pKi)

5-HT1A Receptor

6.5 (pKi)

5-HT2A Receptor

6.4 (pkB)

In Vitro

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 Related Antibodies
In Vivo

GR127935 (10-300 μg/kg, p.o., once) dose-dependently inhibits GR56764-induced contralateral rotations in guinea-pigs, with ID50 of 28 μg/kg[1].
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.

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]
Dosage: 10, 30, 100, 300 μg/kg
Administration: p.o., once
Result: Inhibited GR56764-induced contralateral rotations in guinea-pigs, with ID50 of 28 μg/kg.
Animal Model: Adult male NMRI mice (25-30 g, 5-8 weeks old)[2]
Dosage: 0.005, 0.05, 0.5 ng/mouse
Administration: intra-CA1, 5 min before training
Result: Impaired memory acquisition as shown by decreased step-down latency in the one-trial step-down passive avoidance task.
Molecular Weight

497.59

Formula

C29H31N5O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0097 mL 10.0484 mL 20.0969 mL
5 mM 0.4019 mL 2.0097 mL 4.0194 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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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GR127935 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GR127935148672-13-3GR 127935GR-1279355-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1D5-HT1B receptorneurological diseaseorally activeInhibitorinhibitorinhibit

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