| 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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| Targets |
RY785 (CAS#: 1393748-80-5) targets Kv2.1 (IC50 = 0.05 μM) and Kv2.2 (IC50 = 0.09 μM). [1]
RY785 targets voltage-gated potassium channels KV2.1 and KV2.2. It inhibits KV2.2 with an IC50 of 50 nM (0.05 µM) and KV2.1 with an IC50 of 0.05 µM. The compound displays over 100-fold selectivity for KV2.1 over Cav1.2 calcium channels (IC50 = 17 µM). |
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| ln Vitro |
RY785 (CAS#: 1393748-80-5) inhibits Kv2.1 with an IC50 of 0.05 μM as measured by automated electrophysiology (IonWorks Quattro) at pulse 40 of a 5-Hz train. [1]
It inhibits Kv2.2 with an IC50 of 0.09 μM. [1] Selectivity over Kv1.2: IC50 >10 μM. [1] Activity on CaV1.2: IC50 = 17 μM; on CaV2.3: IC50 >10 μM. [1] No significant activity on CaV2.1, CaV2.2 (IC50 >10 μM), or NaV1.5 and NaV1.7 (IC50 >10 μM for both). [1] The fast-eluting enantiomer (RY785) has IC50 of 0.05 μM on Kv2.1; the slow-eluting enantiomer has IC50 of 0.07 μM. [1] RY785 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with an IC50 of 0.05 µM for KV2.2. It displays over 100-fold selectivity for KV2.1 over Cav1.2 calcium channels (IC50 = 17 µM). The compound has analgesic activity. |
| ln Vivo |
RY785 has analgesic activity and may be used in pain relief studies. By inhibiting KV2 channels, it modulates neuronal excitability and reduces pain signaling. The compound's selectivity for KV2 over Cav1.2 calcium channels is an important feature for its safety profile.
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| Enzyme Assay |
Cell-free assays for RY785 utilize purified KV2.2 or KV2.1 channels reconstituted into lipid bilayers or liposomes. Channel activity is measured using voltage-clamp electrophysiology or ion flux assays with fluorescent K+-sensitive dyes. The compound is applied at various concentrations, and inhibition of K+ current is measured. IC50 values are determined from concentration-response curves.
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| Cell Assay |
Cells expressing KV2.2 or KV2.1 channels (e.g., HEK293 cells transfected with the channel) are subjected to whole-cell patch-clamp electrophysiology. K+ currents are elicited by depolarizing voltage steps, and the effect of RY785 on current amplitude is measured at various concentrations. Selectivity over Cav1.2 calcium channels is assessed in cells expressing the calcium channel.
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| Animal Protocol |
In vivo animal studies for RY785 are conducted in rodent models of pain (e.g., formalin test, von Frey test, hot plate test). The compound is administered via intraperitoneal or intrathecal routes. Pain responses are measured and compared to vehicle controls. Dose-response relationships are established to determine ED50 values for analgesic efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RY785 have not been comprehensively reported. As a small molecule (MW 392.47, formula C21H20N4O2S) with moderate lipophilicity, it is expected to have reasonable membrane permeability and potential for central nervous system penetration. The compound is soluble in DMSO. Detailed PK parameters remain to be determined.
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| Toxicity/Toxicokinetics |
RY785 (CAS#: 1393748-80-5) was developed as part of a structure-activity relationship study to reduce calcium channel activity compared to earlier compounds A1 and B1. It is a first (fast) eluting enantiomer from chiral column separation of a racemic mixture. [1]
Toxicity data for RY785 are limited. As a KV2 channel inhibitor, standard toxicological assessments would be required for development. The compound's selectivity for KV2 over Cav1.2 calcium channels (>100-fold) suggests a favorable off-target safety profile. However, KV2 channels are widely expressed in the brain and heart, so on-target effects on neuronal and cardiac function need to be carefully evaluated. |
| References | |
| Additional Infomation |
RY785 (molecular formula C21H20N4O2S, MW 392.47) is a potent and selective voltage-gated potassium (KV2) channel inhibitor. It has analgesic activity and may be used in pain relief studies. The compound displays over 100-fold selectivity for KV2.1 over Cav1.2 calcium channels. It is intended for research use only.
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| Molecular Formula |
C21H20N4O2S
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|---|---|
| Molecular Weight |
392.474102973938
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| Exact Mass |
392.13
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| Elemental Analysis |
C, 64.27; H, 5.14; N, 14.28; O, 8.15; S, 8.17
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| CAS # |
1393748-80-5
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| PubChem CID |
74891293
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
537
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CC1=CC(=CC=C1)OC)C(=O)NC2=CC3=C(C=C2)N=C(N3)C4=CSC=N4
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| InChi Key |
BRHVBJUDTWQELF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N4O2S/c1-13(8-14-4-3-5-16(9-14)27-2)21(26)23-15-6-7-17-18(10-15)25-20(24-17)19-11-28-12-22-19/h3-7,9-13H,8H2,1-2H3,(H,23,26)(H,24,25)
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| Chemical Name |
3-(3-methoxyphenyl)-2-methyl-N-[2-(1,3-thiazol-4-yl)-3H-benzimidazol-5-yl]propanamide
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| Synonyms |
RY-785; RY785; RY 785;
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~254.80 mM)
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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 | 2.5480 mL | 12.7398 mL | 25.4797 mL | |
| 5 mM | 0.5096 mL | 2.5480 mL | 5.0959 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5480 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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