SQ28603 (SQ28,603) (Synonyms: SQ28,603; Squibb 28603) |
| Katalog-Nr.GC31583 |
SQ28603 (SQ28,603) ist ein potenter und selektiver Inhibitor der neutralen Endopeptidase 3.4.24.11 (NEP), einem Enzym, das das atriale natriuretische Peptid (ANP) abbaut.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 100845-83-8
Sample solution is provided at 25 µL, 10mM.
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SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
In conscious deoxycorticosterone acetate (DOCA)/salt hypertensive rats, 300 μmol/kg, i.v., of SQ28603 significantly lowers mean arterial pressure (MAP) from 177±12 to 154±8 mm Hg and increases urinary cyclic guanosine monophosphate (GMP) excretion from 204±70 to 1,068±326 pmol/kg/min within 2 h. SQ28603 also significantly reduces NEP activity by 95% in the kidneys (1.28±0.08 vs. 18.35±0.61 μmol/min after SQ28603 and vehicle respectively) and by 77% in the lungs (0.29±0.03 vs. 0.92±0.14 μmol/kg after SQ28603 and vehicle, respectively). In conclusion, inhibition of NEP activity by SQ28603 significantly decreases MAP and increases plasma ANP concentrations and urinary excretion of cyclic GMP in conscious DOCA/salt hypertensive rats[1]. The potent neutral endopeptidase inhibitor SQ28603 significantly increases excretion of sodium from 4.9±2.3 to 14.3±2.1 muequiv./min and cyclic 3',5'-guanosine monophosphate from 118±13 to 179±18 pmol/min after intravenous administration of 300 μmol/kg (approximately 80 mg/kg) in conscious female cynomolgus monkeys[2].
[1]. Seymour AA, et al. Antihypertensive and renal activity of SQ 28,603, an inhibitor of neutral endopeptidase. J Cardiovasc Pharmacol. 1991 Feb;17(2):296-304. [2]. Seymour AA, et al. Evaluation of SQ 28,603, an inhibitor of neutral endopeptidase, in conscious monkeys. Can J Physiol Pharmacol. 1991 Oct;69(10):1609-17.
| Cas No. | 100845-83-8 | SDF | |
| Überlieferungen | SQ28,603; Squibb 28603 | ||
| Canonical SMILES | OC(CCNC(C(CS)CC1=CC=CC=C1)=O)=O | ||
| Formula | C13H17NO3S | M.Wt | 267.34 |
| Löslichkeit | Soluble in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7406 mL | 18.7028 mL | 37.4056 mL |
| 5 mM | 0.7481 mL | 3.7406 mL | 7.4811 mL |
| 10 mM | 0.3741 mL | 1.8703 mL | 3.7406 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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