| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary target of Olodanrigan sodium is the angiotensin II type 2 receptor (AT2R). It acts as a highly selective and peripherally restricted antagonist of AT2R. By blocking AT2R, it inhibits AngII/AT2R-induced activation of p38 and p42/p44 MAPK, thereby reducing DRG neuron hyperexcitability and sprouting. This contributes to its analgesic effects in neuropathic pain.
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| ln Vitro |
In vitro, Olodanrigan sodium is a highly selective AT2R antagonist. Its activity is typically measured using radioligand binding assays with cell membranes expressing AT2R and functional assays that assess its ability to block AT2R-mediated signaling (e.g., MAPK activation).
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| ln Vivo |
On day 14 following chronic traumatic injury (CCI), EMA401 sodium (10 mg/kg; neck) significantly enhances theta power and paw withdrawal latency (PWL) [4].
In vivo, Olodanrigan sodium is orally active and peripherally restricted. It has potential for the treatment of postherpetic neuralgia (PHN) and other neuropathic pain conditions. Its efficacy in animal models of neuropathic pain has been demonstrated. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Olodanrigan sodium involve radioligand binding studies using cell membranes expressing AT2R. Competitive binding assays are performed using a radiolabeled AT2R ligand to determine the compound's affinity (Ki) for the receptor. Its selectivity for AT2R over AT1R and other receptors is assessed.
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| Cell Assay |
In vitro cellular assays for Olodanrigan sodium are conducted in cells expressing AT2R, such as DRG neurons. Cells are treated with the compound, and its ability to inhibit AngII-induced MAPK activation is assessed by western blotting. Its effects on neuronal hyperexcitability and sprouting are measured using electrophysiological and morphological techniques.
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| Animal Protocol |
In vivo animal studies for Olodanrigan sodium are conducted in animal models of neuropathic pain, such as the spinal nerve ligation model or postherpetic neuralgia model. Animals are administered the compound orally, and pain behavior (e.g., mechanical allodynia, thermal hyperalgesia) is assessed. Its effects on DRG neuron hyperexcitability and sprouting are evaluated by histological and electrophysiological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Olodanrigan sodium indicate it is orally bioavailable and peripherally restricted. Its peripheral restriction limits central nervous system side effects. Its molecular weight and formula are not specified in the available snippets, but it is a sodium salt of Olodanrigan.
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| Toxicity/Toxicokinetics |
Toxicological information for Olodanrigan sodium is derived from preclinical studies. As an AT2R antagonist, it is generally well tolerated. Peripheral restriction may limit central side effects. Comprehensive toxicology studies would be required for clinical development, including assessments of its effects on blood pressure and renal function.
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| References | |
| Additional Infomation |
Olodanrigan is being investigated in the clinical trial NCT03297294 (Safety and efficacy of EMA401 in patients with diabetic neuropathic pain (PDN)).
Olodanrigan sodium is a highly selective AT2R antagonist being developed for the treatment of neuropathic pain. It is also known as PD-126055 and EMA-401. It is orally bioavailable and peripherally restricted. It has potential for the treatment of postherpetic neuralgia. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C32H28NNAO5
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|---|---|
| Molecular Weight |
530.566139936447
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| Exact Mass |
529.186
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| CAS # |
1316755-17-5
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| Related CAS # |
Olodanrigan;1316755-16-4
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| PubChem CID |
9937291
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
752
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[Na+].O(CC1C=CC=CC=1)C1=C(C=CC2=C1CC(C(=O)O)N(C(C(C1C=CC=CC=1)C1C=CC=CC=1)=O)C2)OC
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| InChi Key |
AKMGNOBRQGBYJM-YCBFMBTMSA-M
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| InChi Code |
InChI=1S/C32H29NO5.Na/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)/q+1/p-1/t27-/m0./s1
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| Chemical Name |
Sodium (3S)-2-(2,2-Diphenylacetyl)-6-methoxy-5-phenylmethoxy-3,4-dihydro-1H-isoquinoline-3-carboxylate
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| Synonyms |
EMA401 PD-126055EMA-401 PD 126055EMA 401 EMA401 sodium PD126055
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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) |
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
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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 | 1.8848 mL | 9.4238 mL | 18.8477 mL | |
| 5 mM | 0.3770 mL | 1.8848 mL | 3.7695 mL | |
| 10 mM | 0.1885 mL | 0.9424 mL | 1.8848 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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