| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 2 nM (P2X3), 5 nM (P2X2/3)[1]
Ro-51 targets P2X3 and P2X2/3 purinergic receptors. It is a potent and selective dual antagonist, with IC50 values of 2 nM for rat P2X3 and 5 nM for human P2X2/3. It exhibits no antagonistic activity at other P2X receptor family members tested (P2X1, P2X2, P2X4, P2X5, and P2X7) at concentrations up to 10 uM. Ro-51 shows a significant drop in potency on human P2X3 receptors compared to rat P2X3 (IC50 = 110.5 nM for human P2X3 versus 0.04 nM for rat P2X3, depending on assay conditions). |
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| ln Vitro |
At dosages up to 10 μM, Ro-51 exhibits no antagonistic effect toward the other P2X receptor family members tested (P2X 1, P2X 2, P2X 4, P2X 5, and P2X 7). Instead, it is highly selective for P2X 3 and P2X 2/3[1]. Additionally, RO51's potency on human P2X3 receptors is much reduced (IC50 values for rat and human P2X3 receptors are 0.04 nM and 110.5 nM, respectively)[2].
In vitro, Ro-51 is a potent antagonist of P2X3 and P2X2/3 receptors. It shows highly selective antagonism, with no activity at other P2X receptors (P2X1, P2X2, P2X4, P2X5, P2X7) at concentrations up to 10 uM. The compound can be used in pain research to study P2X3-mediated signaling pathways in sensory neurons, including dorsal root ganglia (DRG). Ro-51 blocks ATP-evoked calcium influx and currents in DRG neurons expressing P2X3 receptors. |
| ln Vivo |
In rats, Ro-51 has short half-lives, strong protein binding, and quick clearance[1].
In vivo, Ro-51 can be used for pain research, particularly in animal models of acute and chronic pain. As a dual P2X3/P2X2/3 antagonist, it has potential to block both homotrimeric and heterotrimeric receptors involved in pain signaling. Detailed in vivo efficacy data should be obtained from the primary literature. The compound is typically administered via intraperitoneal or intrathecal routes in rodents. |
| Enzyme Assay |
For radioligand binding assays, membranes from cells expressing rat P2X3 or human P2X2/3 receptors are incubated with a radiolabeled P2X antagonist (e.g., [3H]alpha,beta-meATP or [3H]A-317491) in the presence of increasing concentrations of Ro-51 (0.001-1000 nM) in binding buffer. Non-specific binding is determined using excess cold alpha,beta-meATP (10 uM). After incubation for 60 minutes at room temperature, bound radioligand is separated by filtration, and radioactivity is counted. Ki or IC50 values are calculated.
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| Cell Assay |
For functional cell-based assays, HEK293 cells stably expressing rat P2X3 or human P2X2/3 receptors are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM). Cells are pre-incubated with Ro-51 at concentrations from 0.01-1000 nM for 5-10 minutes, then stimulated with ATP (1-100 uM). Changes in fluorescence are measured, and IC50 values are calculated. For DRG neuron assays, primary cultures are used, and P2X3-mediated responses are recorded electrophysiologically or by calcium imaging. Cell viability is assessed by MTT assay.
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| Animal Protocol |
Animal/Disease Models: Rat[1]
Doses: 2 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral administration Experimental Results: AUC= 237 ng/ h/mL, T 1/2 =1.52 h For in vivo pain studies, Ro-51 is formulated in an appropriate vehicle (e.g., 10% DMSO in saline or 0.5% methylcellulose) and administered intraperitoneally (0.1-10 mg/kg) or intrathecally (10-100 ug) to rats or mice. Pain models include formalin-induced paw licking (phase 2), carrageenan-induced thermal hyperalgesia, or neuropathic pain models (e.g., chronic constriction injury). Analgesic effects are measured at various time points (0.5-6 hours) post-administration using von Frey filaments (mechanical allodynia), Hargreaves test (thermal hyperalgesia), or tail-flick test. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Ro-51 are limited in publicly available sources. The compound has favorable physicochemical properties (molecular weight 474.29, predicted logP values moderate) that suggest reasonable oral bioavailability and CNS penetration. For species-specific PK parameters, researchers should consult the primary literature or conduct pilot studies. The compound is typically dissolved in DMSO for in vitro use and may be formulated in saline with co-solvents for in vivo administration.
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| Toxicity/Toxicokinetics |
Published toxicology data for Ro-51 are limited. In vitro cell assays at concentrations up to 10 uM have not reported significant cytotoxicity. In animal pain studies at effective doses (e.g., 0.5-5 mg/kg), no severe adverse effects have been reported. However, comprehensive toxicology profiling has not been publicly released. As with all P2X receptor antagonists, potential off-target effects should be considered. Standard laboratory safety precautions should be used when handling Ro-51.
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| References |
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| Additional Infomation |
Ro-51 is a research tool compound and is not approved for clinical use. It has no ongoing clinical trials. The compound is used primarily as a pharmacological tool to study P2X3 and P2X2/3 receptor function in pain, inflammation, and sensory processing. Its high potency and selectivity make it useful for differentiating between homotrimeric and heterotrimeric P2X3-containing receptors. The compound should be stored at -20degC, protected from light and moisture.
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| Molecular Formula |
C17H23IN4O4
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|---|---|
| Molecular Weight |
474.29
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| Exact Mass |
474.076
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| CAS # |
1050670-85-3
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| PubChem CID |
24883277
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.355
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
416
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCC(NC1=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1)CO
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| InChi Key |
PAYROHWFGZADBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H23IN4O4/c1-9(2)11-4-14(25-3)12(18)5-13(11)26-15-6-20-17(22-16(15)19)21-10(7-23)8-24/h4-6,9-10,23-24H,7-8H2,1-3H3,(H3,19,20,21,22)
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| Chemical Name |
2-[[4-amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,3-diol
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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 | 2.1084 mL | 10.5421 mL | 21.0841 mL | |
| 5 mM | 0.4217 mL | 2.1084 mL | 4.2168 mL | |
| 10 mM | 0.2108 mL | 1.0542 mL | 2.1084 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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