Sparsentan (RE-021) |
| رقم الكتالوجGC32479 |
Sparsentan (RE-021) (RE-021) هو مضاد قوي لمستقبلات الأنجيوتنسين II و endothelin A مع Kis من 0.8 و 9.3 نانومتر ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 254740-64-2
Sample solution is provided at 25 µL, 10mM.
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Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 value of 0.8 µmol/kg iv and 3.6 µmol/kg po. Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model. Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10 µmol/kg/day) in spontaneously hypertensive rats. Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. At 100 µmol/kg/day, Sparsentan reduces the blood pressure from 170 to less than 100 mmHg during the course of the drug's pharmacokinetic duration. Sparsentan at 100 µmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration[1].
[1]. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
Animal experiment: | Rats: Rats are gavaged with vehicle, and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response. Irbesartan (30 µmol/kg) and Sparsentan (30 µmol/kg) are given by oral gavage (po), and the rats are re-challenged with angiotensin II at various intervals up to 240 min. There are 6-8 rats per drug dose. The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect[1]. |
References: [1]. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. | |
| Cas No. | 254740-64-2 | SDF | |
| Canonical SMILES | O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2COCC)(NC5=NOC(C)=C5C)=O | ||
| Formula | C32H40N4O5S | M.Wt | 592.75 |
| الذوبان | DMSO: 250 mg/mL (421.76 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 1.6871 mL | 8.4353 mL | 16.8705 mL |
| 5 mM | 0.3374 mL | 1.6871 mL | 3.3741 mL |
| 10 mM | 0.1687 mL | 0.8435 mL | 1.6871 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 ddH2O, 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
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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