Granisetron hydrochloride

CAS No. 107007-99-8

Granisetron hydrochloride( BRL 43694 )

Catalog No. M10289 CAS No. 107007-99-8

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
25MG 46 In Stock
50MG 67 In Stock
100MG 116 In Stock
200MG 169 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    Granisetron hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  • Description
    Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. IC50 Value: 17uM (GR reduced 5-HT-evoked contractions)(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.(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. 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.
  • 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.
  • 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. 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.
  • Synonyms
    BRL 43694
  • Pathway
    Endocrinology/Hormones
  • Target
    5-HT Receptor
  • Recptor
    5-HT
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    107007-99-8
  • Formula Weight
    348.87
  • Molecular Formula
    C18H25ClN4O
  • Purity
    >98% (HPLC)
  • Solubility
    Ethanol: 1 mg/mL (2.86 mM); Water: 70 mg/mL (200.64 mM); DMSO: 1 mg/mL (2.86 mM)
  • SMILES
    Cl.CN1N=C(C(=O)NC2CC3CCCC(C2)N3C)C2=CC=CC=C12
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Turvill JL, et al. Br J Pharmacol. 2000 Jul;130(5):1031-6.
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