| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
HP210 is a selective, small-molecule modulator of the Glucocorticoid Receptor (GR). It acts as a SGRM, which allows it to selectively modulate GR activity, potentially dissociating the desired anti-inflammatory effects from the unwanted metabolic side effects typical of traditional glucocorticoids.
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| ln Vitro |
In vitro studies demonstrate that HP210 inhibits NF-kappaB (a key pro-inflammatory transcription factor) transcriptional activity with an IC50 of 1.92 microM. It also effectively suppresses the transcription of multiple pro-inflammatory genes induced by LPS, such as IL-1beta, IL-6, and COX-2.Importantly, it shows no toxicity to mouse fibroblast 3T3 cells at effective doses.
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| ln Vivo |
In vivo data for HP210 are currently limited and not publicly detailed. As a selective GR modulator (SGRM), it is being researched for its potential to treat inflammatory diseases by modulating GR activity with a superior safety profile compared to classical steroidal glucocorticoids.
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| Enzyme Assay |
Cell-free NF-kappaB transcription assays are performed to assess its impact on GR activity. Nuclear extracts containing activated NF-kappaB are incubated with a biotinylated NF-kappaB consensus oligonucleotide. The compound‘s effect is measured using an ELISA-based kit designed to quantify the degree of NF-kappaB activation via its binding to the immobilized oligonucleotide sequence.
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| Cell Assay |
Cellular anti-inflammatory assays use mouse fibroblast 3T3 cells. Cells are pre-treated with HP210 and then stimulated with Lipopolysaccharide (LPS) to induce inflammation. The gene expression levels of key cytokines (IL-1beta and IL-6) and inflammatory enzymes (COX-2) are measured via quantitative real-time PCR to evaluate the compound's inhibitory effect on the inflammatory cascade.
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| Animal Protocol |
In vivo data is not available for this compound. As a laboratory chemical, it is not typically formulated for animal pharmacokinetic or efficacy studies in a standard research setting.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties are not documented. As a laboratory chemical primarily for in vitro use, ADME (Absorption, Distribution, Metabolism, Excretion) data are not typically required or reported.
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| Toxicity/Toxicokinetics |
Based on available data, HP210 exhibits a favorable safety profile in cell-based systems. No significant toxicity was observed in mouse fibroblast 3T3 cells at concentrations that effectively inhibited the inflammatory response, suggesting a good therapeutic window.
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| References | |
| Additional Infomation |
HP210 is a selective GR modulator (SGRM) chemical probe. Unlike full agonists that cause widespread gene activation and side effects, SGRMs like HP210 are designed to provide a more targeted modulation of the receptor for inflammatory diseases. It is a research compound and has not been approved for clinical use.
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| Molecular Formula |
C22H19N3O2S2
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|---|---|
| Molecular Weight |
421.535162210464
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| Exact Mass |
421.091
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| CAS # |
728039-52-9
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| Related CAS # |
S-HP210;R-HP210
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| PubChem CID |
4362044
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1=CC=CC=C1)NC(=O)C2=CC=C(C=C2)CN3C(=O)C4=C(C=CS4)NC3=S
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| InChi Key |
AJJBGZJAGZSMJI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19N3O2S2/c1-14(16-5-3-2-4-6-16)23-20(26)17-9-7-15(8-10-17)13-25-21(27)19-18(11-12-29-19)24-22(25)28/h2-12,14H,13H2,1H3,(H,23,26)(H,24,28)
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| Chemical Name |
4-[(4-oxo-2-sulfanylidene-1H-thieno[3,2-d]pyrimidin-3-yl)methyl]-N-(1-phenylethyl)benzamide
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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: 125 mg/mL (296.53 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 | 2.3723 mL | 11.8613 mL | 23.7225 mL | |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL | |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 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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