EMA401 (Synonyms: EMA401; PD-126055) |
| رقم الكتالوجGC19137 |
EMA401 (EMA401) هو مناهض لمستقبلات الأنجيوتنسين 2 من النوع 2 (AT2R) انتقائي للغاية ونشط عن طريق الفم ومقيد محيطيًا.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1316755-16-4
Sample solution is provided at 25 µL, 10mM.
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EMA401, a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.target: AT2RIn vivo: AngII induces p38, p42/p44 mitogen activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons that is blocked by EMA401. Inhibits capsaicin responses in cultured hDRG neurons.
References:
[1]. Rice AS et al. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.Lancet. 2014 May 10;383(9929):1637-47.
[2]. Anand U et al. Mechanisms underlying clinical efficacy of Angiotensin II type 2 receptor (AT2R) antagonist EMA401 in neuropathic pain: clinical tissue and in vitro studies. Mol Pain. 2015 Jun 26;11:38.
[3]. Rice AS et al. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.Lancet. 2014 May 10;383(9929):1637-47.
| Cas No. | 1316755-16-4 | SDF | |
| المرادفات | EMA401; PD-126055 | ||
| Canonical SMILES | O=C([C@H]1N(C(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC4=C(C(OCC5=CC=CC=C5)=C(OC)C=C4)C1)O | ||
| Formula | C32H29NO5 | M.Wt | 507.58 |
| الذوبان | DMSO : ≥ 34 mg/mL (66.98 mM) | Storage | Store at -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 | 1.9701 mL | 9.8507 mL | 19.7013 mL |
| 5 mM | 0.394 mL | 1.9701 mL | 3.9403 mL |
| 10 mM | 0.197 mL | 0.9851 mL | 1.9701 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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
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- 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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