| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
|
|---|---|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information on the use of granisetron during lactation. Until more data becomes available, granisetron should be used with caution during lactation. Alternative medications are recommended. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk A woman who breastfed an 8-month-old infant 6 to 8 times daily was admitted for an appendectomy. During the surgery, she received granisetron, cefazolin, ketorolac, rocuronium bromide, succinylcholine, and sufentanil. The patient also received two intravenous boluses of 150 mg propofol, followed shortly by an intravenous bolus of 50 mg propofol. Postoperatively, she took acetaminophen, cefazolin, ibuprofen, and pantoprazole, and oxycodone and dimenhydrinate as needed. Twenty-two hours post-surgery, the mother expressed breast milk for the first time and found it to be light green. Analysis of the green milk using an unverified testing method yielded no detectable propofol. The green color gradually faded, disappearing completely by the time she resumed breastfeeding on the fourth day post-surgery. The authors suggest that the green color was likely caused by propofol or its metabolites. |
| References |
|
| Additional Infomation |
1-Methyl-N-{9-methyl-9-azabicyclo[3.3.1]nonane-3-yl}-1H-indazole-3-carboxamide belongs to the indazole class of compounds and is an aromatic amide. It is a selective serotonin receptor (5HT-3) antagonist and has been used as an antiemetic for cancer chemotherapy patients. See also: granisetron (note moved to).
|
| Molecular Formula |
C18H21D3N4O
|
|---|---|
| Molecular Weight |
315.435
|
| Exact Mass |
312.195
|
| CAS # |
1224925-64-7
|
| Related CAS # |
Granisetron;109889-09-0;Granisetron-d3 (1-methyl-d3);1224925-76-1
|
| PubChem CID |
3510
|
| Appearance |
Typically exists as solid at room temperature
|
| Melting Point |
219 °C (hydrochloride salt)
|
| LogP |
2.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
23
|
| Complexity |
442
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MFWNKCLOYSRHCJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)
|
| Chemical Name |
1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1702 mL | 15.8509 mL | 31.7017 mL | |
| 5 mM | 0.6340 mL | 3.1702 mL | 6.3403 mL | |
| 10 mM | 0.3170 mL | 1.5851 mL | 3.1702 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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