Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Olodanrigan (EMA-401; PD-126055; EMA401) is a novel, orally bioavailable, peripherally restricted and highly selective AT2R (angiotensin II type 2 receptor) antagonist that can be potentially used for treatment of postherpetic neuralgia (PHN). Decreased hyperexcitability and DRG neuron sprouting are prevented by inhibiting augmented AngII/AT2R-induced p38 and p42/p44 MAPK activation. As a treatment for neuropathic pain, it is currently under development.
Targets |
AT2R
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ln Vitro |
EMA401 may work through intracrine or paracrine processes at peripheral nerve terminals to lessen the signaling of neuropathic pain in AngII/NGF/TRPV1-convergent pathways.[1]
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ln Vivo |
EMA401, at day 14, rats treated with a selective small molecule AT2R antagonist exhibit a significant reduction in theta power and an increase in paw withdrawal latencies (PWL) following chronic constriction injury (CCI).[2]
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Cell Assay |
Duplicate plates were plated for 48 hours, and then treated for 30 minutes at 37 °C with AngII (10 nM), AngII + EMA401 (10 and 100 nM, respectively), 100 nM EMA401, NGF (100 ng/ml), or the vehicle treatment (control 0). After that, the dishes were fixed for 30 minutes with 4% PFA in preparation for immunostaining.
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Animal Protocol |
Adult male Sprague-Dawley (SD) rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve
1 mg/kg (i.v.); 10 mg/kg (p.o.) i.v.; p.o. |
References |
Molecular Formula |
C32H29NO5
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Molecular Weight |
507.5764
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Exact Mass |
507.2
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Elemental Analysis |
C, 75.72; H, 5.76; N, 2.76; O, 15.76
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CAS # |
1316755-16-4
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Related CAS # |
Olodanrigan sodium; 1316755-17-5; 1348410-84-3 (potasium)
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Appearance |
Solid powder
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SMILES |
COC1=C(C2=C(CN([C@@H](C2)C(=O)O)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4)C=C1)OCC5=CC=CC=C5
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InChi Key |
GHBCIXGRCZIPNQ-MHZLTWQESA-N
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InChi Code |
InChI=1S/C32H29NO5/c1-37-28-18-17-25-20-33(31(34)29(23-13-7-3-8-14-23)24-15-9-4-10-16-24)27(32(35)36)19-26(25)30(28)38-21-22-11-5-2-6-12-22/h2-18,27,29H,19-21H2,1H3,(H,35,36)/t27-/m0/s1
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Chemical Name |
(3S)-2-(2,2-diphenylacetyl)-6-methoxy-5-phenylmethoxy-3,4-dihydro-1H-isoquinoline-3-carboxylic acid
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Synonyms |
EMA 401; PD-126055; EMA401; PD 126055; EMA-401; EMA-401 potasium; PD126055 potasium
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~197.0 mM)
Ethanol: ~100 mg/mL |
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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 | 1.9701 mL | 9.8507 mL | 19.7013 mL | |
5 mM | 0.3940 mL | 1.9701 mL | 3.9403 mL | |
10 mM | 0.1970 mL | 0.9851 mL | 1.9701 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.
Diagram indicating the pathway involved in AngII and TRPV1 signalling, with activation of p38 (MAPK) and p44/42 (ERK) and their inhibition by EMA401 in DRG neurons. Mol Pain . 2015 Jun 26:11:38. td> |
Pain Med . 2013 May;14(5):692-705. td> |