Seglitide acetate
Based on 1 Customer Validation
Seglitide acetate (MK-678 acetate) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide acetate also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide acetate produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide acetate inhibits glucagon secretion and reduces circulating insulin levels. Seglitide acetate causes a sustained, reversible reduction in elevated systolic blood pressure in Streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide acetate induces membrane hyperpolarization and inhibits electrical excitability. Seglitide acetate induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide acetate can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus.
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- Pureté : 98.76%
- CAS No.: 99248-33-6
- Formule: C46H60N8O9
- Masse moléculaire:869.02
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Cortistatin-14Somatostatin Receptor Inhibitor
Activité biologique
Description
IC50 & Target
[1]|
SSTR2 |
In Vivo
Seglitide (50-100 µg/rat/day; p.o.; daily; 49 days) acetate produces only a transient 11% reduction in systolic blood pressure in male spontaneously hypertensive rats, with no sustained hypotensive effect, and no impact on relevant hormones, renin-angiotensin system components, blood glucose, or growth rate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, streptozotocin-induced diabetic hypertension)[2]
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Dosage:50 µg/rat/day (days 1-20); 100 µg/rat/day (days 21-49); 1000 µg/rat/day; 100 µg (acute parenteral)
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Administration:p.o. (via drinking water, days 1-20); p.o. (via drinking water, days 21-49); p.o. (unspecified duration); parenteral (single acute dose)
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Result:Reduced systolic blood pressure of diabetic rats by 14% after 17 days of 50 µg/rat/day treatment (P=0.05).
Maintained systolic blood pressure significantly reduced by 11-21% relative to untreated diabetic rats over days 24-49 with 100 µg/rat/day dose, matching normotensive control levels (98-118 mmHg; repeated measures ANOVA, P<0.003 vs. untreated diabetic rats, P=0.687 vs. normal rats).
Reversed hypotensive effect 5 days after drug withdrawal, with only a 6% reduction in blood pressure (nsd).
Showed no significant effect on plasma renin activity, angiotensin converting enzyme activity, or aldosterone levels in diabetic rats.
Did not alter circulating insulin or glucagon levels in diabetic rats with 1000 µg/rat/day oral dose, but reduced circulating insulin levels by 44% with acute parenteral 100 µg dose (P<0.05).
Had no significant effect on blood glucose levels or growth rate of diabetic rats over 49 days of treatment.
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Animal Model:Spontaneously hypertensive (SH) (male)[2]
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Dosage:50 µg/rat/day (days 1-40); 100 µg/rat/day (days 41-49)
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Administration:p.o. (via drinking water, days 1-40); p.o. (via drinking water, days 41-49)
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Result:Reduced systolic blood pressure of SH rats by 11% at the 10-day time point (P<0.02), with no significant blood pressure reduction observed in subsequent measurements even after dose escalation to 100 µg/rat/day.
Showed no significant effect on plasma renin activity, angiotensin converting enzyme activity, or aldosterone levels in SH rats.
Did not alter blood glucose levels or growth rate of SH rats over 49 days of treatment.
Chemical Information
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CAS No. 99248-33-6
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Appearance Solid
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Masse moléculaire 869.02
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Formule C46H60N8O9
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Color White to off-white
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Synonyms
MK 678 acetate; L 36358 acetate
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Sequence
Cyclo({Ala(Me)}-Tyr-{d-Trp}-Lys-Val-Phe)
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Sequence Shortening
Cyclo({Ala(Me)}-Y-{d-Trp}-KVF)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (115.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (295 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dimech J, et al. Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria. Br J Pharmacol. 1993;109(4):898-899. [Content Brief]
[2]. Hartmann J, et al. Blood pressure reduction in hypertensive-diabetic rats by the somatostatin analog MK-678. Life Sci. 1989;45(3):267-274. [Content Brief]
[3]. Bhattarai JP, et al. Somatostatin inhibition of gonadotropin-releasing hormone neurons in female and male mice. Endocrinology. 2010 Jul;151(7):3258-66. [Content Brief]
[4]. McKeen ES, et al. Mediation by SRIF1 receptors of the contractile action of somatostatin in rat isolated distal colon; studies using some novel SRIF analogues. Br J Pharmacol. 1994;113(2):628-634. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.1507 mL | 5.7536 mL | 11.5072 mL | 28.7680 mL |
| 5 mM | 0.2301 mL | 1.1507 mL | 2.3014 mL | 5.7536 mL | |
| 10 mM | 0.1151 mL | 0.5754 mL | 1.1507 mL | 2.8768 mL | |
| 15 mM | 0.0767 mL | 0.3836 mL | 0.7671 mL | 1.9179 mL | |
| 20 mM | 0.0575 mL | 0.2877 mL | 0.5754 mL | 1.4384 mL | |
| 25 mM | 0.0460 mL | 0.2301 mL | 0.4603 mL | 1.1507 mL | |
| 30 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9589 mL | |
| 40 mM | 0.0288 mL | 0.1438 mL | 0.2877 mL | 0.7192 mL | |
| 50 mM | 0.0230 mL | 0.1151 mL | 0.2301 mL | 0.5754 mL | |
| 60 mM | 0.0192 mL | 0.0959 mL | 0.1918 mL | 0.4795 mL | |
| 80 mM | 0.0144 mL | 0.0719 mL | 0.1438 mL | 0.3596 mL | |
| 100 mM | 0.0115 mL | 0.0575 mL | 0.1151 mL | 0.2877 mL |
Seglitide acetate Related Classifications
HY-106103A Related Classifications
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Keywords
- Seglitide
- 99248-33-6
- MK 678
- L 36358
- MK678
- MK-678
- L36358
- L-36358
- Somatostatin Receptor
- spontaneously hypertensive rats
- guinea-pig isolated right atria
- somatostatin receptor subtype 2
- GnRH neurons
- carbachol
- N6-cyclohexyladenosine
- streptozotocin-diabetic rats
- female mice
- male mice
- rat isolated distal colon
- Inhibitor
- inhibitor
- inhibit