HSR6071 |
Catalog No.GC32056
One-Click Copy Product Info
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HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 111374-21-1
Sample solution is provided at 25 µL, 10mM.
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HSR6071 is an antiallergic agent with potential for the treatment of asthma.
HSR-6071 suppresses antigen-induced histamine and SRS-A release from minced lung tissues of guinea-pigs sensitized passively with rabbit anti-EA serum and is a more potent inhibitor of the release of SRS-A than of histamine. On the other hand, histamine- or acetylcholine-induced bronchoconstriction in guinea-pigs is scarcely affected by HSR-6071 at doses sufficient to inhibit the experimental asthma, but LTD4-induced bronchoconstriction is dramatically inhibited. HSR-6071 inhibits cyclic AMP phosphodiesterase activity and produces relaxation of the guinea-pig isolated trachea[1]. HSR-6071 inhibits the IgE-mediated histamine release with an IC50 of 0.46 nM. HSR-6071 is effective not only by i.v. but also by p.o. administration on the IgE mediated PCA in rats. The most potent inhibition with HSR-6071 is observed when it is given p.o. 5 min before the antigen challenge, indicating the rapid absorption of HSR-6071 through the gastrointestinal tract[2].
[1]. Makino E, et al. Inhibitory effect of HSR-6071, a new anti-allergic agent, on experimental asthma in rats and guinea-pigs. J Pharm Pharmacol. 1990 Apr;42(4):236-41. [2]. Makino E, et al. Potent inhibitory activity of HSR-6071, a new antiallergic agent, on passive cutaneousanaphylaxis (PCA). Jpn J Pharmacol. 1990 Jan;52(1):87-94.
Animal experiment: | Rats: In order to find out the proper pre treatment time with HSR-6071, 0.03 mg/kg, i.vi or 1 mg/kg, p.o. of HSR-6071 was given at varying times before the antigen challenge[2]. |
References: [1]. Makino E, et al. Inhibitory effect of HSR-6071, a new anti-allergic agent, on experimental asthma in rats and guinea-pigs. J Pharm Pharmacol. 1990 Apr;42(4):236-41. | |
| Cas No. | 111374-21-1 | SDF | |
| Canonical SMILES | O=C(C1=NC(N2CCCC2)=CN=C1)NC3=NN=NN3 | ||
| Formula | C10H12N8O | M.Wt | 260.26 |
| Solubility | H2O : 50 mg/mL (192.12 mM; ultrasonic and adjust pH to 12 with NaOH) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8423 mL | 19.2116 mL | 38.4231 mL |
| 5 mM | 768.5 μL | 3.8423 mL | 7.6846 mL |
| 10 mM | 384.2 μL | 1.9212 mL | 3.8423 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)