1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. GR 125743

GR 125743 

Cat. No.: HY-121392 Purity: 99.78%
Handling Instructions

GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases.

For research use only. We do not sell to patients.

GR 125743 Chemical Structure

GR 125743 Chemical Structure

CAS No. : 148547-33-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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Description

GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases[1][2].

IC50 & Target[1]

human 5-HT1B Receptor

8.85 (pKi)

human 5-HT1D Receptor

8.31 (pKi)

In Vitro

GR 125743 has a Kd of 0.61 nM for h5-HT1B[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GR 125743 (0.3 mg/kg; i.p.) produces significant decreases in extracellular 5-HT in the frontal cortex of the conscious guinea pig[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Dunkin Hartley guinea-pigs (350–450 g)[2]
Dosage: 0.3 mg/kg
Administration: Intraperitoneal injection
Result: Produced significant transient increases in extracellular 5-HT.
Molecular Weight

416.52

Formula

C₂₅H₂₈N₄O₂

CAS No.

148547-33-5

SMILES

O=C(C1=CC=C(C(C)=C1)C2=CC=NC=C2)NC3=CC=C(C(N4CCN(CC4)C)=C3)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4008 mL 12.0042 mL 24.0085 mL
5 mM 0.4802 mL 2.4008 mL 4.8017 mL
10 mM 0.2401 mL 1.2004 mL 2.4008 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GR 125743GR125743GR-1257435-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorh5-HT1Breceptorh5-HT1DParkinson's diseasecognitive disordercardiovascularInhibitorinhibitorinhibit

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GR 125743
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HY-121392
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