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| Targets |
HSR6071 targets the IgE-mediated allergic response pathway. It strongly inhibits IgE-mediated histamine release from mast cells and basophils. It also inhibits cyclic AMP phosphodiesterase activity, contributing to bronchodilation and relaxation of airway smooth muscle.
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| ln Vitro |
In vitro, HSR6071 inhibits IgE-mediated histamine release with an IC50 of 0.46 nM. It inhibits cyclic AMP phosphodiesterase activity and induces relaxation of isolated guinea pig trachea. These mechanisms contribute to its anti-allergic and bronchodilatory effects.
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| ln Vivo |
In rats with experimental asthma brought on by IgE antibodies, HSR-6071 (0.01-0.1 mg/kg; iv) suppresses the condition in a dose-dependent way. In addition, HSR-6071 (0.3, 1.3 mg/kg; intravenously) inhibits guinea pigs' IgE or IgG antibody-mediated bronchoconstriction. The isolated trachea of guinea pigs is relaxed by HSR-6071, which also suppresses the activity of cyclic AMP phosphodiesterase [1]. HSR-6071 has an IC50 of 0.46 nM, which suppresses IgE-mediated histamine release. Both oral and intravenous treatment of HSR-6071 effectively inhibits IgE-mediated PCA in rats. HSR-6071 rapidly absorbs via the gastrointestinal tract, as evidenced by the most effective inhibitory effect reported when the drug was taken orally five minutes prior to antigen presentation [2].
In vivo, HSR6071 (0.01-0.1 mg/kg, intravenous) dose-dependently inhibits IgE antibody-induced experimental asthma in rats. It also prevents IgE- or IgG-mediated bronchoconstriction in guinea pigs at 0.3-1.3 mg/kg (intravenous). Oral administration 5 minutes before antigen challenge shows maximal inhibitory effect, indicating rapid gastrointestinal absorption. |
| Enzyme Assay |
In vitro receptor binding assays for HSR6071 are not typically performed, as its mechanism involves inhibition of histamine release and phosphodiesterase activity rather than direct receptor antagonism. Phosphodiesterase enzyme assays are conducted using purified PDE enzymes and appropriate substrates, with activity measured by colorimetric or luminescence-based methods.
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| Cell Assay |
Cellular assays for HSR6071 are conducted using mast cells or basophils. Cells are sensitized with IgE and challenged with antigen in the presence of serial dilutions of HSR6071 (0.01-100 nM). Histamine release is measured by ELISA or fluorometric methods. IC50 values are calculated from dose-response curves. Cell viability is assessed to ensure non-cytotoxic concentrations.
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| Animal Protocol |
In vivo studies for HSR6071 are conducted in rat models of experimental asthma and passive cutaneous anaphylaxis (PCA). The compound is administered via intravenous or oral routes. For PCA, the compound is given before antigen challenge, and skin reactions are measured. For asthma models, airway resistance and inflammatory cell infiltration are assessed.
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| ADME/Pharmacokinetics |
Dosing schedules and routes are optimized based on the model.
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| Toxicity/Toxicokinetics |
Pharmacokinetic properties of HSR6071 include rapid gastrointestinal absorption following oral administration. The compound has a molecular weight of 260.26 and formula C10H12N8O. It is soluble in water (20 mg/mL). It is stored at -20degC for long-term stability. Detailed PK parameters such as half-life and bioavailability are available in preclinical study reports.
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| References |
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| Additional Infomation |
Toxicological data for HSR6071 indicate that it is well-tolerated at pharmacologically active doses. No significant toxicity has been reported in preclinical studies. Standard toxicology assessments include evaluation of body weight, organ function, and histopathology in animal models.
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| Molecular Formula |
C10H12N8O
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|---|---|
| Molecular Weight |
260.25528
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| Exact Mass |
260.113
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| CAS # |
111374-21-1
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| PubChem CID |
159466
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.555g/cm3
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| Index of Refraction |
1.717
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| LogP |
-0.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LUJDHCXCWJFNOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12N8O/c19-9(13-10-14-16-17-15-10)7-5-11-6-8(12-7)18-3-1-2-4-18/h5-6H,1-4H2,(H2,13,14,15,16,17,19)
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| Chemical Name |
6-pyrrolidin-1-yl-N-(2H-tetrazol-5-yl)pyrazine-2-carboxamide
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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) |
H2O : ~50 mg/mL (~192.12 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 | 3.8423 mL | 19.2116 mL | 38.4231 mL | |
| 5 mM | 0.7685 mL | 3.8423 mL | 7.6846 mL | |
| 10 mM | 0.3842 mL | 1.9212 mL | 3.8423 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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