Seglitide
Based on 1 Customer Validation
Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide 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 produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide 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 induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.30%
- CAS 番号: 81377-02-8
- 分子式: C44H56N8O7
- 分子量:808.96
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保管条件:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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SSTR2 |
Seglitide (50-100 µg/rat/day; p.o.; daily; 49 days) 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.
化学情報
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CAS 番号 81377-02-8
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性状 Solid
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分子量 808.96
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分子式 C44H56N8O7
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Color White to off-white
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別名
MK-678; L-363586
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配列
Cyclo({Ala(Me)}-Tyr-{d-Trp}-Lys-Val-Phe)
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シーケンスの短縮
Cyclo({Ala(Me)}-Y-{d-Trp}-KVF)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
純度とドキュメンテーション
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データシート (264 KB)
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SDS (252 KB)
- English - EN (252 KB)
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- Deutsch - DE (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Seglitide 関連分類
HY-106103 関連分類
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- Seglitide
- 81377-02-8
- MK-678
- L-363586
- MK678
- MK 678
- L363586
- L 363586
- L-363586
- 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