| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
RdRP-IN-2 targets RNA-dependent RNA polymerase (RdRp). By inhibiting RdRp, the compound reduces viral load and mitigates the severity of infections caused by RNA viruses. It has shown potential activity against a range of RNA viruses, including coronaviruses and flaviviruses.
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|---|---|
| ln Vitro |
RdRP-IN-2 (Compound 17) totally prevents Feline Coronavirus (FIPV) and SARS-CoV-2 from replicating. Vero and CRFK cells do not respond cytotoxically to RdRP-IN-2[1]. In Vero cells, RdRP-IN-2 (Compound 17) demonstrates anti-SARS-CoV-2 activity with an EC50 value of 527.3 nM[1].
RdRP-IN-2 significantly inhibits SARS-CoV-2 RdRp with an IC50 of 41.2 μM. It completely inhibits SARS-CoV-2 and feline coronavirus (FIPV) replication. The compound shows no cytotoxicity to Vero and CRFK cells. |
| ln Vivo |
RdRP-IN-2 has shown potential activity against a range of RNA viruses. By inhibiting RdRp, the compound interferes with viral genome synthesis and reduces viral load without affecting host cellular processes.
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| Enzyme Assay |
RdRp inhibition assays are performed using recombinant SARS-CoV-2 RdRp. RdRP-IN-2 is incubated with the enzyme and a template-primer, and inhibition of RNA synthesis is measured. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based antiviral assays are conducted using Vero and CRFK cells infected with SARS-CoV-2 or FIPV. Cells are treated with RdRP-IN-2, and viral replication is measured. Cytotoxicity is assessed to confirm selectivity.
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| Animal Protocol |
In vivo studies for RdRP-IN-2 are not extensively reported. As a research compound for RNA virus inhibition, its primary use is in vitro. Future studies could involve animal models of coronavirus infection.
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| ADME/Pharmacokinetics |
RdRP-IN-2 has a molecular formula of C17H13BrF3N5O3S2. Storage: standard conditions for research compounds.
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| Toxicity/Toxicokinetics |
RdRP-IN-2 is a research compound not intended for human use. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Milan Dejmek, et al. Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication. Viruses. 2021 Aug 11;13(8):1585.
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| Additional Infomation |
RdRP-IN-2 is a small molecule RNA-dependent RNA polymerase (RdRp) inhibitor. It significantly inhibits SARS-CoV-2 RdRp (IC50 = 41.2 μM) and FIPV replication. It is used for research on RNA viruses.
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| Exact Mass |
566.188
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|---|---|
| CAS # |
2863657-16-1
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| PubChem CID |
156613478
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| Appearance |
Light yellow to green yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CCC(CC1)OC2=CC3=C(C=C2)SC4=C(C=C(C(=O)N34)C5=CC=CC=C5)C(=O)N[C@@H](CC6=CC=CC=C6)C(=O)O
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| InChi Key |
BQZJTBOLNKPLGS-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C33H30N2O5S/c36-30(34-27(33(38)39)18-21-10-4-1-5-11-21)26-20-25(22-12-6-2-7-13-22)31(37)35-28-19-24(16-17-29(28)41-32(26)35)40-23-14-8-3-9-15-23/h1-2,4-7,10-13,16-17,19-20,23,27H,3,8-9,14-15,18H2,(H,34,36)(H,38,39)/t27-/m0/s1
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| Chemical Name |
(2S)-2-[(8-cyclohexyloxy-1-oxo-2-phenylpyrido[2,1-b][1,3]benzothiazole-4-carbonyl)amino]-3-phenylpropanoic acid
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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 (176.47 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.) |
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.
Products are for research use only; We do not sell to patients
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