WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526606
CAS#: 142999-59-5
Description: GYKI-46903 is a non-competitive antagonist for 5-HT3 receptors. In displacement studies, the pIC50 values of GYKI-46903 against [3H]granisetron binding to rat cerebral cortex membranes were 6.91. GYKI-46903, when administered by intravenous infusion, antagonized the decrease in heart rate evoked by serotonin (Bezold-Jarisch reflex) in anaesthetized rats, and the maximal reversal was less than 50%.
Hodoodo Cat#: H526606
Name: GYKI-46903 HCl
CAS#: 142999-59-5
Chemical Formula: C17H21ClFNO2
Exact Mass: 0.00
Molecular Weight: 325.808
Elemental Analysis: C, 62.67; H, 6.50; Cl, 10.88; F, 5.83; N, 4.30; O, 9.82
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Synonym: GYKI-46903; GYKI 46903; GYKI46903; GYKI-46,903; GYKI 46,903; GYKI46,903.
IUPAC/Chemical Name: (4R,5R)-6-(4-fluorophenyl)-1-azabicyclo[3.3.1]non-6-en-4-yl propionate hydrochloride
InChi Key: UBIAWBSPCYNXMC-IDVLALEDSA-N
InChi Code: InChI=1S/C17H20FNO2.ClH/c1-2-17(20)21-16-8-10-19-9-7-14(15(16)11-19)12-3-5-13(18)6-4-12;/h3-7,15-16H,2,8-11H2,1H3;1H/t15-,16+;/m0./s1
SMILES Code: FC1=CC=C(C2=CCN3CC[C@@H](OC(CC)=O)[C@H]2C3)C=C1.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 325.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Maksay G, Bíró T, Bugovics G. Allosteric modulation of 5-HT3 serotonin receptors. Eur J Pharmacol. 2005 May 2;514(1):17-24. Epub 2005 Apr 22. PubMed PMID: 15878320.
2: Vitális B, Sebestyén L, Sike M, Sólyom S, Hársing LG Jr. Binding characteristics of GYKI-46 903, a non-competitive ligand at 5-HT3 receptors. Pharmacol Res. 2001 Mar;43(3):291-9. PubMed PMID: 11401422.
3: Bagdy E, Solyom S, Harsing LG Jr. Feedback stimulation of somatodendritic serotonin release: a 5-HT3 receptor-mediated effect in the raphe nuclei of the rat. Brain Res Bull. 1998;45(2):203-8. PubMed PMID: 9443841.
4: Csillik-Perczel V, Bakonyi A, Yemane T, Vitalis B, Horvath E, Solyom S, Szekely JI, Harsing LG Jr. GYKI-46 903, a non-competitive antagonist for 5-HT3 receptors. Pharmacol Toxicol. 1996 Jul;79(1):32-9. PubMed PMID: 8841094.