1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Granisetron Hydrochloride

Granisetron Hydrochloride (Synonyms: BRL 43694A)

Cat. No.: HY-B0071A Purity: 99.69%
Handling Instructions

Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

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

Granisetron Hydrochloride Chemical Structure

Granisetron Hydrochloride Chemical Structure

CAS No. : 107007-99-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
Estimated Time of Arrival: December 31
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Description

Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

IC50 & Target

5-HT3 Receptor

17 μM (IC50)

In Vitro

In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT[1].

In Vivo

Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion[2]. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation[3].

Clinical Trial
Molecular Weight

348.87

Formula

C₁₈H₂₅ClN₄O

CAS No.

107007-99-8

SMILES

CN1N=C(C(N[[email protected]]2C[[email protected]](N3C)CCC[[email protected]]3C2)=O)C4=CC=CC=C41.[H]Cl

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 : 7.69 mg/mL (22.04 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8664 mL 14.3320 mL 28.6640 mL
5 mM 0.5733 mL 2.8664 mL 5.7328 mL
10 mM 0.2866 mL 1.4332 mL 2.8664 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: ≥ 0.77 mg/mL (2.21 mM); Clear solution

  • 2.

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

    Solubility: ≥ 0.77 mg/mL (2.21 mM); Clear solution

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

GranisetronBRL 43694A5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Granisetron Hydrochloride
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