Emedastine-13C-d3 (fumarate) |
| رقم الكتالوجGC49063 |
An internal standard for the quantification of emedastine
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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Emedastine-13C-d3 is intended for use as an internal standard for the quantification of emedastine by GC- or LC-MS. Emedastine is a histamine H1 receptor antagonist (Ki = 1.3 nM).1 It is selective for histamine H1 over H2 and H3 receptors (Kis = 49 and 12.43 µM, respectively), as well as α1-, α2-, and β1-adrenergic and dopamine D1 and D2 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1 and 5-HT2 at 10 µM.1,2 Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).3 It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC50s = 2.23, 3.42, and 1.50 nM, respectively).4 Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs.2 Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
1.Sharif, N.A., Su, S.X., and Yanni, J.M.Emedastine: A potent, high affinity histamine H1-receptor-selective antagonist for ocular use: Receptor binding and second messenger studiesJ. Ocul. Pharmacol.10(4)653-664(1994) 2.Yanni, J.M., Stephens, D.J., Parnell, D.W., et al.Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular useJ. Ocul. Pharmacol.10(4)665-675(1994) 3.Sharif, N.A., Xu, S.X., Magnino, P.E., et al.Human conjunctival epithelial cells express histamine-1 receptors coupled to phosphoinositide turnover and intracellular calcium mobilization: Role in ocular allergic and inflammatory diseasesExp. Eye Res.63(2)169-178(1996) 4.Weimer, L.K., Gamache, D.A., and Yanni, J.M.Histamine-stimulated cytokine secretion from human conjunctival epithelial cells: Inhibition by the histamine H1 antagonist emedastineInt. Arch. Allergy. Immunol.115(4)288-293(1998)
| Cas No. | N/A | SDF | |
| Canonical SMILES | CCOCCN1C2=CC=CC=C2N=C1N3CCCN([13C]([2H])([2H])[2H])CC3.OC(/C=C/C(O)=O)=O | ||
| Formula | C16[13C]H23D3N4O·C4H4O4 | M.Wt | 422.5 |
| الذوبان | Acetonitrile: soluble,DMSO: soluble,Methanol: soluble | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3669 mL | 11.8343 mL | 23.6686 mL |
| 5 mM | 0.4734 mL | 2.3669 mL | 4.7337 mL |
| 10 mM | 0.2367 mL | 1.1834 mL | 2.3669 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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