Emedastine
Based on 1 publication(s) in Google Scholar
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.02%
- CAS 番号: 87233-61-2
- 分子式: C17H26N4O
- 分子量:302.41
-
保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-B0801
FexofenadineH1R Antagonist -
HY-12542
DantroleneDlutathione Reductase Inhibitor -
HY-17043
LoratadineInfluenza Virus Inhibitor -
HY-10230
MidostaurinMulti-targeted Protein Kinase Inhibitor -
HY-B1033
Metergoline5-HT/Dopamine Receptors Antagonist -
HY-B1296
PromethazineH1 Receptor Antagonist -
HY-B1339
Dicyclomine hydrochlorideM1/2 Muscarinic Receptor Antagonist -
HY-14896
OpicaponeCOMT Inhibitor -
HY-I0021
BepotastineHistamine H1 Receptor Antagonist -
HY-108411R
Emedastine (Standard)Histamine H1 Receptor Antagonist -
HY-B0640
EpinastineHistamine H1 Receptor Antagonist -
HY-12190
JNJ-5207852Histamine Receptor Antagonist
MedChemExpress（MCE）の使用を引用している文献 Emedastine
MoreHistamine Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
H1 Receptor 1.3 nM (Ki) |
H2 Receptor 49067 nM (Ki) |
H3 Receptor 12430 nM (Ki) |
体外実験
Emedastine inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1].
High concentrations of Emedastine (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2].
Emedastine (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3].
Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2].
Emedastine inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male ICR mice 5-6 weeks of age[3]
-
Dosage:0.03, 0.1, 0.3 mg/kg
-
Administration:Orally; 30 min before pruritogen injection
-
Result:Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 87233-61-2
-
性状 Viscous Liquid
-
分子量 302.41
-
分子式 C17H26N4O
-
Color Yellow to brown
-
SMILES
CN1CCN(C2=NC3=CC=CC=C3N2CCOCC)CCC1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (413.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 100 mg/mL (330.68 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (277 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64. [Content Brief]
[2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. [Content Brief]
[3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL | 82.6692 mL |
| 5 mM | 0.6614 mL | 3.3068 mL | 6.6135 mL | 16.5338 mL | |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3068 mL | 8.2669 mL | |
| 15 mM | 0.2205 mL | 1.1023 mL | 2.2045 mL | 5.5113 mL | |
| 20 mM | 0.1653 mL | 0.8267 mL | 1.6534 mL | 4.1335 mL | |
| 25 mM | 0.1323 mL | 0.6614 mL | 1.3227 mL | 3.3068 mL | |
| 30 mM | 0.1102 mL | 0.5511 mL | 1.1023 mL | 2.7556 mL | |
| 40 mM | 0.0827 mL | 0.4133 mL | 0.8267 mL | 2.0667 mL | |
| 50 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.6534 mL | |
| 60 mM | 0.0551 mL | 0.2756 mL | 0.5511 mL | 1.3778 mL | |
| 80 mM | 0.0413 mL | 0.2067 mL | 0.4133 mL | 1.0334 mL | |
| 100 mM | 0.0331 mL | 0.1653 mL | 0.3307 mL | 0.8267 mL |
Emedastine 関連分類
HY-108411 関連分類
Powered by Bioz